Indazolesulfonylurea derivative, its use and intermediate for its production

ABSTRACT

The present invention provides an indazolesulfonylurea derivative represented by the general formula: ##STR1## [wherein R 1  is a hydrogen atom or an alkyl group, etc., R 2  and R 3  are the same or different and represent a hydrogen atom, a halogen atom, an alkyl group, the formula --COR 4  (wherein R 4  represents an alkoxy group, etc.), an alkoxy group, a haloalkoxy group or a cyano group, etc., X is an oxygen atom or a sulfur atom, Y is a hydrogen atom or an alkyl group, etc., A and B are the same or different and represent a halogen atom, an alkoxy group or an alkyl group, etc., and Z represents a nitrogen atom or a methine group], as well as a herbicide containing it as an active ingredient and an intermediate for its production. 
     The compound of the present invention exhibits excellent herbicidal effects over a wide range from the preemergence stage to the growing stage of various weeds which are problematic in agricultural fields. Further, it is capable of controlling weeds germinating in paddy fields.

TECHNICAL FIELD

The present invention relates to a novel indazolesulfonylurea derivative(hereinafter referred to as a compound of the present invention), anintermediate for its production and a herbicide containing it as anactive ingredient.

BACKGROUND ART

Heretofore, many sulfonylurea derivatives such as sulfometuron-methylhave been known as herbicides. Japanese Unexamined Patent PublicationNo. 95091/1992 discloses a herbicide containing an indazolesulfonylureaas an active ingredient. However, the compound of the present inventioni.e. a sulfonylurea derivative having a sulfamoyl group substituted atthe 3-position of an indazole ring, has not been known. Further, theintermediate for its production i.e. an indazolesulfonamide derivative,has also not been known.

It is known that sulfonylurea derivatives have herbicidal activities,but such compounds are not necessarily practically satisfactory, forexample, in that their herbicidal effects are inadequate.

Under these circumstances, the present inventors have conducted variousstudies, and as a result, they have found that the compound of thepresent invention is an excellent herbicide having a high activity andhas finally accomplished the present invention.

DISCLOSURE OF THE INVENTION

Namely, the present invention provides an indazolesulfonylureaderivative represented by the general formula: ##STR2## {wherein R¹ is ahydrogen atom, an alkyl group, a cycloalkyl group, a haloalkyl group, analkoxyalkyl group, a benzyloxyalkyl group, a benzyl group, a phenylgroup, a pyridyl group, a dialkylaminocarbonyl group, an alkoxycarbonylgroup, an alkylsulfonyl group, a phenylsulfonyl group, adialkylaminosulfonyl group, a haloalkylcarbonyl group, an alkylcarbonylgroup, a benzoyl group or an alkenyl group, R² and R³ are the same ordifferent and represent a hydrogen atom, a halogen atom, an alkyl group,a cycloalkyl group, an alkenyl group, an alkoxycarbonylalkenyl group, analkynyl group, a haloalkyl group, an alkoxyalkyl group, analkoxycarbonylalkyl group, an alkylcarbonylalkyl group, acycloalkylcarbonylalkyl group, a cyanoalkyl group, adialkylaminocarbonylalkyl group, a dialkylaminoalkyl group, adialkylaminosulfonylalkyl group, an azidoalkyl group, a benzyl group, aphenyl group, a nitro group, a cyano group, an azide group, an aminogroup, a monoalkylamino group, a dialkylamino group, a benzylaminogroup, an alkylcarbonylamino group which may be substituted by a halogenatom, a benzoylamino group, an alkoxycarbonylamino group, aphenoxycarbonylamino group, an alkylsulfonylamino group wherein theamino group may be substituted by an alkyl group, a phenylsulfonylaminogroup wherein the amino group may be substituted by an alkyl group, analkylideneamino group, a benzylideneamino group, a tetrazolyl groupwhich may be substituted, a group represented by the formula --COR⁴(wherein R⁴ is a hydrogen atom, a hydroxyl group, an alkyl group, acycloalkyl group, a haloalkyl group, an alkenyl group, an alkynyl group,a benzyl group, a phenyl group, an alkoxy group, a haloalkoxy group, analkoxyalkoxy group, an alkenyloxy group, a haloalkenyloxy group, analkynyloxy group, a benzyloxy group or a phenoxy group), a grouprepresented by the formula --C(O)NR⁵ R⁶ (wherein R⁵ and R⁶ are the sameor different and represent a hydrogen atom, an alkyl group, an alkenylgroup, an alkynyl group, a benzyl group, a phenyl group or an alkoxygroup), a group represented by the formula --SR⁷ (wherein R⁷ is ahydrogen atom, an alkyl group or a haloalkyl group), a group representedby the formula --SO₂ NR⁵ R⁶ (wherein R⁵ and R⁶ have the same meanings asdefined above), a group represented by the formula --S(O)_(n) R⁸(wherein n represents an integer of 1 or 2, and R⁸ represents an alkylgroup, an alkenyl group or a haloalkyl group), a group represented bythe formula --OR⁹ [wherein R⁹ is a hydrogen atom, an alkyl group, acycloalkylalkyl group, an alkenyl group, an alkynyl group, a benzylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), a haloalkyl group, a haloalkenyl group, a phenylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), an alkoxyalkyl group, an alkoxyalkoxyalkyl group, ahaloalkoxyalkyl group, a benzyloxyalkyl group, a phenoxyalkyl group, analkylthioalkyl group, a dialkylaminoalkyl group, an azidoalkyl group, analkylcarbonyl group, a haloalkylcarbonyl group, a benzoyl group, adialkylaminocarbonyl group, a cyanoalkyl group, an alkylideneaminogroup, a dialkylideneamino group, a benzylideneamino group or analkoxycarbonylalkyl group], or the formula --C(═NOR¹⁰)R¹¹ (wherein R¹⁰represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynylgroup, a benzyl group, a haloalkyl group or a phenyl group, and R¹¹represents a hydrogen atom, an alkyl group, a benzyl group, a haloalkylgroup or a phenyl group), R² and R³ may together form a ring with analkyl group which may contain a hetero atom, A and B are the same ordifferent and represent an alkyl group, a haloalkyl group, an alkoxygroup, a monoalkylamino group, a dialkylamino group, a halogen atom or ahaloalkoxy group, Z represents a methine group or a nitrogen atom, Xrepresents an oxygen atom or a sulfur atom, and Y represents a hydrogenatom, an alkyl group or an alkoxyalkyl group, as well as itsintermediate represented by an indazolesulfonamide derivativerepresented by the formula [I-a] or [II-a]: ##STR3## {wherein R¹ is ahydrogen atom, an alkyl group, a cycloalkyl group, a haloalkyl group, analkoxyalkyl group, a benzyloxyalkyl group, a benzyl group, a phenylgroup, a pyridyl group, a dialkylaminocarbonyl group, an alkoxycarbonylgroup, an alkylsulfonyl group, a phenylsulfonyl group, adialkylaminosulfonyl group, a haloalkylcarbonyl group, an alkylcarbonylgroup, a benzoyl group or an alkenyl group, R² and R³ are the same ordifferent and represent a hydrogen atom, a halogen atom, an alkyl group,a cycloalkyl group, an alkenyl group, an alkoxycarbonylalkenyl group, analkynyl group, a haloalkyl group, an alkoxyalkyl group, analkoxycarbonylalkyl group, an alkylcarbonylalkyl group, acycloalkylcarbonylalkyl group, a cyanoalkyl group, adialkylaminocarbonylalkyl group, a dialkylaminoalkyl group, adialkylaminosulfonylalkyl group, an azidoalkyl group, a benzyl group, aphenyl group, a nitro group, a cyano group, an azide group, an aminogroup, a monoalkylamino group, a dialkylamino group, a benzylaminogroup, an alkylcarbonylamino group which may be substituted by a halogenatom, a benzoylamino group, an alkoxycarbonylamino group, aphenoxycarbonylamino group, an alkylsulfonylamino group wherein theamino group may be substituted by an alkyl group, a phenylsulfonylaminogroup wherein the amino group may be substituted by an alkyl group, analkylideneamino group, a benzylideneamino group, a tetrazolyl groupwhich may be substituted, a group represented by the formula --COR⁴(wherein R⁴ is a hydrogen atom, a hydroxyl group, an alkyl group, acycloalkyl group, a haloalkyl group, an alkenyl group, an alkynyl group,a benzyl group, a phenyl group, an alkoxy group, a haloalkoxy group, analkoxyalkoxy group, an alkenyloxy group, a haloalkenyloxy group, analkynyloxy group, a benzyloxy group or a phenoxy group), a grouprepresented by the formula --C(O)NR⁵ R⁶ (wherein R⁵ and R⁶ are the sameor different and represent a hydrogen atom, an alkyl group, an alkenylgroup, an alkynyl group, a benzyl group, a phenyl group or an alkoxygroup), a group represented by the formula --SR⁷ (wherein R⁷ is ahydrogen atom, an alkyl group or a haloalkyl group), a group representedby the formula --SO₂ NR⁵ R⁶ (wherein R⁵ and R⁶ have the same meanings asdefined above), a group represented by the formula --S(O)_(n) R⁸(wherein n represents an integer of 1 or 2, and R⁸ represents an alkylgroup, an alkenyl group or a haloalkyl group), a group represented bythe formula --OR⁹ [wherein R⁹ is a hydrogen atom, an alkyl group, acycloalkylalkyl group, an alkenyl group, an alkynyl group, a benzylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), a haloalkyl group, a haloalkenyl group, a phenylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), an alkoxyalkyl group, an alkoxyalkoxyalkyl group, ahaloalkoxyalkyl group, a benzyloxyalkyl group, a phenoxyalkyl group, analkylthioalkyl group, a dialkylaminoalkyl group, an azidoalkyl group, analkylcarbonyl group, a haloalkylcarbonyl group, a benzoyl group, adialkylaminocarbonyl group, a cyanoalkyl group, an alkylideneaminogroup, a dialkylideneamino group, a benzylideneamino group or analkoxycarbonylalkyl group], or the formula -- C(═NOR¹⁰)R¹¹ (wherein R¹⁰represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynylgroup, a benzyl group, a haloalkyl group or a phenyl group, and R¹¹represents a hydrogen atom, an alkyl group, a benzyl group, a haloalkylgroup or a phenyl group), and R² and R³ may form a ring with an alkylgroup which may contain a hetero atom}, and a herbicide containing theindazolesulfonylurea as an active ingredient.

The compound of the present invention includes a tautomer, a geometricalisomer and an optical isomer thereof.

In the present invention, the alkyl group means a straight chain orbranched chain alkyl group having from 1 to 30 carbon atoms andincludes, for example, a methyl group, an ethyl group, a n-propyl group,an isopropyl group, a n-butyl group, an isobutyl group, a sec-butylgroup, a t-butyl group, a n-pentyl group, an isoamyl group, a neopentylgroup, a n-hexyl group, an isohexyl group, a 3,3-dimethylbutyl group, an-heptyl group, a 5-methylhexyl group, a 4-methylhexyl group, a3-methylhexyl group, a 4,4-dimethylpentyl group, a n-octyl group, a6-methylheptyl group, a n-nonyl group, a 7-methyloctyl group, a n-decylgroup, a 8-methylnonyl group, a n-undecyl group, a 9-methyldecyl group,a n-dodecyl group, a 10-methylundecyl group, a n-tridecyl group, a11-methyldodecyl group, a n-tetradecyl group, a 12-methyltridecyl group,a n-pentadecyl group, a 13-methyltetradecyl group, a n-hexadecyl group,a n-heptadecyl group, a n-octadecyl group, a n-nonadecyl group, and an-eicosyl group.

The alkoxy group and the alkylsulfonyl group mean an (alkyl)--O-- groupand (alkyl)--SO₂ -- group, respectively, in which the alkyl moiety hasthe above-mentioned meaning.

The halogen atom includes fluorine, chlorine, bromine and iodine atoms.

The alkenyl group means a straight chain or branched chain alkenyl grouphaving from 2 to 20 carbon atoms and includes, for example, a vinylgroup, a propenyl group, an isopropenyl group, a butenyl group, apentenyl group, a hexenyl group, a heptenyl group, an octenyl group, a3-methyl-1-butenyl group, and a 4-methyl-1-pentenyl group.

The alkynyl group means a straight chain or branched chain alkynyl grouphaving from 2 to 20 carbon atoms and includes, for example, an ethynylgroup, a propynyl group, a butynyl group, a pentynyl group, a hexynylgroup, a 3,3-dimethyl-1-butynyl group, a 4-methyl-1-pentynyl group, a3-methyl-1-pentynyl group, a 5-methyl-1-hexynyl group, a4-methyl-1-hexynyl group, a 3-methyl-1-hexynyl group, a heptynyl group,an octynyl group, a nonynyl group, a decynyl group, an undecynyl group,a dodecynyl group, a tridecynyl group, a tetradecynyl group, apentadecynyl group, and a hexadecynyl group.

In the above formula [I] or [II], as a group of compounds showingpreferred herbicidal effects, compounds may be mentioned wherein R¹represents a hydrogen atom, a methyl group or an ethyl group, R² and R³are the same or different and represent a hydrogen atom, a halogen atom,an alkoxycarbonyl group, a dialkylaminocarbonyl group, an alkoxy group,a haloalkoxy group, an alkenyloxy group, a cyano group or atrifluoromethyl group, A and B are the same or different and represent amethoxy group, a methyl group or a haloalkoxy group, Z represents amethine group or a nitrogen atom, X represents an oxygen atom, and Yrepresents a hydrogen atom.

Now, typical specific examples of the compound of the present inventionrepresented by the formula [I] or [II] will be exemplified in Tables 1and 2. The compound numbers will be referred to in the subsequentdescription, and when R¹ represents a hydrogen atom, the compound maytake tautomers represented by the formula [I] and [II].

The following symbols in the Tables in the present specificationrepresent the following groups, respectively.

    ______________________________________                                        Bn: Benzyl group   Pr: n-Propyl group                                         Pen: n-Pentyl group                                                                              Bu: n-Butyl group                                          Me: Methyl group   Ph: Phenyl group                                           Et: Ethyl group                                                               ______________________________________                                    

                                      TABLE 1                                     __________________________________________________________________________     ##STR4##                                                                     Comp.                                                                         No. R.sup.1                                                                             R.sup.2      R.sup.3   X  Y     A   B     Z   mp.                   __________________________________________________________________________                                                            (°C.)          I-1 Me    Ph           H         O  H     OMe OMe   CH                        I-2 Me    Bn           H         O  H     OMe OMe   CH                        I-3 Me    SH           H         O  H     OMe OMe   CH                        I-4 Me    SMe          H         O  H     OMe OMe   CH                        I-5 Me    SEt          H         O  H     OMe OMe   CH  189-190               I-6 Me    SPr          H         O  H     OMe OMe   CH  162-164               I-7 Me    SO.sub.2 Me  H         O  H     OMe OMe   CH                        I-8 Me    SO.sub.2 Et  H         O  H     OMe OMe   CH  157-160               I-9 Me    SOMe         H         O  H     OMe OMe   CH                        I-10                                                                              Me    SO.sub.2 NHMe                                                                              H         O  H     OMe OMe   CH                        I-11                                                                              Me    SO.sub.2 NHOMe                                                                             H         O  H     OMe OMe   CH                        I-12                                                                              Me    SO.sub.2 NMe.sub.2                                                                         H         O  H     OMe OMe   CH  214-216               I-13                                                                              Me    SO.sub.2 NHBn                                                                              H         O  H     OMe OMe   CH                        I-14                                                                              Me    SO.sub.2 NHPh                                                                              H         O  H     OMe OMe   CH                        I-15                                                                              Me    SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                             H         O  H     OMe OMe   CH                        I-16                                                                              Me    SO.sub.2 NHCH.sub.2 CCH                                                                    H         O  H     OMe OMe   CH                        I-17                                                                              H     Cl           H         O  H     OMe OMe   CH  191-193               I-18                                                                              Me    Cl           H         O  H     OMe Me    CH  195-198               I-19                                                                              Me    Cl           5-Cl      O  H     OMe OMe   CH  210-213               I-20                                                                              Et    Cl           H         O  H     OMe OMe   CH  187-189               I-21                                                                              Ph    Cl           H         O  H     OMe OMe   CH                        I-22                                                                              Bn    Cl           H         O  H     OMe OMe   CH                        I-23                                                                              Me    H            H         O  H     OMe OMe   CH  181-183               I-24                                                                              Me    H            H         O  H     OMe Me    CH                        I-25                                                                              Me    H            H         O  H     OMe Me    N   172-174               I-26                                                                              Me    F            H         O  H     OMe OMe   CH  205-209               I-27                                                                              Me    Br           H         O  H     OMe OMe   CH  276-279               I-28                                                                              Me    Me           H         O  H     OMe OMe   CH  178-180               I-29                                                                              Me    CN           H         O  H     OMe OMe   CH  267-269               I-30                                                                              Me    CF.sub.3     H         O  H     OMe OMe   CH                        I-31                                                                              Me    Cl           H         O  H     OMe Me    CH  243-245               I-32                                                                              Me    Cl           H         O  H     OMe Me    N   266-267               I-33                                                                              Me    F            H         O  H     Me  Me    CH  195-197               I-34                                                                              Me    F            H         O  H     OMe Me    N   197-200               I-35                                                                              Me    F            H         O  H     OMe Me    CH  180-185               I-36                                                                              Me    H            5-Cl      O  H     OMe OMe   CH                        I-37                                                                              Me    H            5-Cl      O  H     Me  Me    CH                        I-38                                                                              Me    H            5-Cl      O  H     OMe Me    N                         I-39                                                                              Me    H            6-Cl      O  H     OMe OMe   CH                        I-40                                                                              Me    H            6-Cl      O  H     Me  Me    CH                        I-41                                                                              Me    H            6-Cl      O  H     Me  Me    N                         I-42                                                                              Me    H            7-Cl      O  H     OMe OMe   CH                        I-43                                                                              Me    H            7-Cl      O  H     OMe Me    N                         I-44                                                                              Me    Cl           H         S  H     OMe OMe   CH                        I-45                                                                              Me    Cl           H         O  Me    OMe OMe   CH                        I-46                                                                              Me    COH          H         O  H     OMe OMe   CH                        I-47                                                                              Me    COMe         H         O  H     OMe OMe   CH                        I-48                                                                              Me    COEt         H         O  H     OMe OMe   CH                        I-49                                                                              Me    COPh         H         O  H     OMe OMe   CH                        I-50                                                                              Me    COCH.sub.2 CHCH.sub.2                                                                      H         O  H     OMe OMe   CH                        I-51                                                                              Me    COCH.sub.2 CCH                                                                             H         O  H     OMe OMe   CH                        I-52                                                                              Me    COBn         H         O  H     OMe OMe   CH                        I-53                                                                              Me    NO.sub.2     H         O  H     OMe OMe   CH  219-220               I-54                                                                              Me    NH.sub.2     H         O  H     OMe OMe   CH                        I-55                                                                              Me    NHMe         H         O  H     OMe OMe   CH                        I-56                                                                              Me    NMe.sub.2    H         O  H     OMe OMe   CH                        I-57                                                                              Me    NHCOMe       H         O  H     OMe OMe   CH                        I-58                                                                              Me    NHCOPh       H         O  H     OMe OMe   CH                        I-59                                                                              Me    NHCOCH.sub.2 Cl                                                                            H         O  H     OMe OMe   CH                        I-60                                                                              Me    NHSO.sub.2 CH.sub.3                                                                        H         O  H     OMe OMe   CH                        I-61                                                                              Me    NHSO.sub.2 Ph                                                                              H         O  H     OMe OMe   CH                        I-62                                                                              Me    CO.sub.2 H   H         O  H     OMe OMe   CH                        I-63                                                                              Me    CO.sub.2 Me  H         O  H     OMe OMe   CH  187-190               I-64                                                                              Me    CO.sub. 2 Et H         O  H     OMe OMe   CH  192-195               I-65                                                                              Me    CO.sub.2 Pr  H         O  H     OMe OMe   CH  195-197               I-66                                                                              Me    CO.sub.2 Pr-i                                                                              H         O  H     OMe OMe   CH  168-169               I-67                                                                              Me    CO.sub.2 Bu  H         O  H     OMe OMe   CH  169-172               I-68                                                                              Me    CO.sub.2 Pen H         O  H     OMe OMe   CH                        I-69                                                                              Me    CO.sub.2 Bn  H         O  H     OMe OMe   CH                        I-70                                                                              Me    CO.sub.2 Ph  H         O  H     OMe OMe   CH                        I-71                                                                              Me    CO.sub.2 CH.sub.2 CH.sub.2 F                                                               H         O  H     OMe OMe   CH                        I-72                                                                              Me    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     OMe OMe   CH                        I-73                                                                              Me    CO.sub.2 CH.sub.2 CCH                                                                      H         O  H     OMe OMe   CH                        I-74                                                                              Me    CO.sub.2 Me  H         O  H     OCHF.sub.2                                                                        OCHF.sub.2                                                                          CH                        I-75                                                                              Me    CO.sub.2 Et  H         O  H     OCHF.sub.2                                                                        OCHF.sub.2                                                                          CH                        I-76                                                                              Me    CO.sub.2 Me  H         O  H     OMe Cl    CH                        I-77                                                                              Me    CO.sub.2 Me  H         O  H     OMe Me    CH                        I-78                                                                              Me    CO.sub.2 Me  H         O  H     OMe Me    N                         I-79                                                                              Me    CO.sub.2 Et  H         O  H     OMe Me    N   193-196               I-80                                                                              Me    CO.sub.2 Me  H         O  H     OMe OCHF.sub.2                                                                          CH                        I-81                                                                              Me    CO.sub.2 Me  5-F       O  H     OMe OMe   CH                        I-82                                                                              Et    CO.sub.2 Me  H         O  H     OMe OMe   CH  182-183               I-83                                                                              Bu    CO.sub.2 Me  H         O  H     OMe OMe   CH                        I-84                                                                              Bn    CO.sub.2 Me  H         O  H     OMe OMe   CH                        I-85                                                                              Ph    CO.sub.2 Me  H         O  H     OMe OMe   CH                        I-86                                                                              H     CO.sub.2 Et  H         O  H     OMe OMe   CH                        I-87                                                                              Me    CO.sub.2 Me  H         S  H     OMe OMe   CH                        I-88                                                                              Me    CO.sub.2 Et  H         S  H     OMe OMe   CH                        I-89                                                                              Me    CO.sub.2 Me  H         O  Me    OMe OMe   CH                        I-90                                                                              Me    OH           H         O  H     OMe OMe   CH                        I-91                                                                              Me    OMe          H         O  H     OMe OMe   CH  265-267               I-92                                                                              Me    OEt          H         O  H     OMe OMe   CH  162-164               I-93                                                                              Me    OPr          H         O  H     OMe OMe   CH  134-136               I-94                                                                              Me    OPr-i        H         O  H     OMe OMe   CH  168-171               I-95                                                                              Me    OBu          H         O  H     OMe OMe   CH  198-200               I-96                                                                              Me    OBn          H         O  H     OMe OMe   CH                        I-97                                                                              Me    OBn(4-Cl)    H         O  H     OMe OMe   CH                        I-98                                                                              Me    OBn(3-OMe)   H         O  H     OMe OMe   CH                        I-99                                                                              Me    OBn(2-Me)    H         O  H     OMe OMe   CH                        I-100                                                                             Me    OPh          H         O  H     OMe OMe   CH                        I-101                                                                             Me    OPh(4-Cl)    H         O  H     OMe OMe   CH                        I-102                                                                             Me    OPh(3-OMe)   H         O  H     OMe OMe   CH                        I-103                                                                             Me    OPh(2-Me)    H         O  H     OMe OMe   CH                        I-104                                                                             Me    OCH.sub.2 CHCH.sub.2                                                                       H         O  H     OMe OMe   CH                        I-105                                                                             Me    OCH.sub.2 CCH                                                                              H         O  H     OMe OMe   CH                        I-106                                                                             Me    OCH.sub.2 CF.sub.3                                                                         H         O  H     OMe OMe   CH                        I-107                                                                             Me    OCH.sub.2 CH.sub.2 OMe                                                                     H         O  H     OMe OMe   CH                        I-108                                                                             Me    OCH.sub.2 CH.sub.2 OPh                                                                     H         O  H     OMe OMe   CH                        I-109                                                                             Me    OCOMe        H         O  H     OMe OMe   CH                        I-110                                                                             Me    OMe          H         O  H     OMe Me    CH                        I-111                                                                             Me    OMe          H         O  H     OMe Me    N   269-270               I-112                                                                             Me    OMe          H         O  H     Me  Me    CH  267-268               I-113                                                                             Me    OEt          H         O  H     OMe Cl    CH  161-165               I-114                                                                             Me    OEt          H         O  H     OMe Me    CH  169-170               I-115                                                                             Me    OEt          H         O  H     Me  Me    CH                        I-116                                                                             Me    CONH.sub.2   H         O  H     OMe OMe   CH                        I-117                                                                             Me    CONHMe       H         O  H     OMe OMe   CH                        I-118                                                                             Me    CONHEt       H         O  H     OMe OMe   CH                        I-119                                                                             Me    CONHPr       H         O  H     OMe OMe   CH                        I-120                                                                             Me    CONMe.sub.2  H         O  H     OMe OMe   CH  205-207               I-121                                                                             Me    CONEt.sub.2  H         O  H     OMe OMe   CH                        I-122                                                                             Me    CONHBn       H         O  H     OMe OMe   CH                        I-123                                                                             Me    CONHPh       H         O  H     OMe OMe   CH                        I-124                                                                             Me    CONHCH.sub.2 CHCH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-125                                                                             Me    CONHCH.sub.2 CCH                                                                           H         O  H     OMe OMe   CH                        I-126                                                                             Me    CONHOMe      H         O  H     OMe OMe   CH                        I-127                                                                             Me    H            5-F       O  H     OMe OMe   CH                        I-128                                                                             Me    H            5-F       O  H     Me  Me    CH                        I-129                                                                             Me    H            5-F       O  H     OMe Me    CH                        I-130                                                                             Me    H            5-F       O  H     OMe Me    N                         I-131                                                                             H     COOMe        H         O  H     OMe OMe   CH  179-180               I-132                                                                             H     COOMe        H         O  H     OMe Cl    CH  193-194               I-133                                                                             H     Cl           H         O  H     OMe Cl    CH  178-181               I-134                                                                             Me    Cl           H         O  H     OMe OMe   CH  265-267               I-135                                                                             Me    SO.sub.2 NH.sub.2                                                                          H         O  H     OMe OMe   CH                        I-136                                                                             H     Br           H         O  H     OMe OMe   CH  190-193               I-137                                                                             Me    H            5-OMe     O  H     OMe OMe   CH                        I-138                                                                             Me    H            5-OEt     O  H     OMe OMe   CH                        I-139                                                                             Me    H            5-OPr     O  H     OMe OMe   CH                        I-140                                                                             Me    OCH(CF.sub.3)Me                                                                            H         O  H     OMe OMe   CH                        I-141                                                                             Me    OCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     OMe OMe   CH                        I-142                                                                             Me    OCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe OMe   CH                        I-143                                                                             Me    OCH.sub.2 CH.sub.2 OEt                                                                     H         O  H     OMe OMe   CH                        I-144                                                                             Me    OCH.sub.2 CH.sub.2 OPr-i                                                                   H         O  H     OMe OMe   CH                        I-145                                                                             Me    OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe OMe   CH                        I-146                                                                             Me    OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe OMe   CH                        I-147                                                                             Me    OCH.sub.2 COOEt                                                                            H         O  H     OMe OMe   CH                        I-148                                                                             Me    OCH.sub.2 CH.sub.2 NMe.sub.2                                                               H         O  H     OMe OMe   CH                        I-149                                                                             Me    SBu          H         O  H     OMe OMe   CH  165-168               I-150                                                                             Me    SPr-i        H         O  H     OMe OMe   CH  178-180               I-151                                                                             Me    SO.sub.2 Pr  H         O  H     OMe OMe   CH  163- 167              I-152                                                                             Me    SO.sub.2 Bu  H         O  H     OMe OMe   CH  187-189               I-153                                                                             Me    SO.sub.2 Pr-i                                                                              H         O  H     OMe OMe   CH  279-281               I-154                                                                             Me    NHBn         H         O  H     OMe OMe   CH                        I-155                                                                             Me    NEt.sub.2    H         O  H     OMe OMe   CH                        I-156                                                                             Me    OMe          5-Cl      O  H     OMe OMe   CH                        I-157                                                                             Me    Br           H         O  H     OMe Me    CH  276-279               I-158                                                                             Et    Cl           H         O  H     OMe Me    CH  182-184               I-159                                                                             Ph    Cl           H         O  H     OMe Me    CH                        I-160                                                                             Me    OPr          H         O  H     OMe Me    CH  178-180               I-161                                                                             Me    OBu          H         O  H     OMe Me    CH  174-176               I-162                                                                             Me    OPr-i        H         O  H     OMe Me    CH  184-186               I-163                                                                             Me    H            5-OMe     O  H     OMe Me    CH                        I-164                                                                             Me    H            5-OEt     O  H     OMe Me    CH                        I-165                                                                             Me    H            5-OPr     O  H     OMe Me    CH                        I-166                                                                             Me    OCH.sub.2 CF.sub.3                                                                         H         O  H     OMe Me    CH                        I-167                                                                             Me    OCH(CF.sub.3)Me                                                                            H         O  H     OMe Me    CH                        I-168                                                                             Me    OCH.sub.2 CH.sub.2 OMe                                                                     H         O  H     OMe Me    CH                        I-169                                                                             Me    OCH.sub.2 CH.sub.2 OEt                                                                     H         O  H     OMe Me    CH                        I-170                                                                             Me    OCH.sub.2 CH.sub. 2 OPr-i                                                                  H         O  H     OMe Me    CH                        I-171                                                                             Me    OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe Me    CH                        I-172                                                                             Me    OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe Me    CH                        I-173                                                                             Me    OCH.sub.2 CH.sub.2 NMe.sub.2                                                               H         O  H     OMe Me    CH                        I-174                                                                             Me    SPr          H         O  H     OMe Me    CH  155-156               I-175                                                                             Me    CO.sub.2 Pr  H         O  H     OMe Me    CH  185-186               I-176                                                                             Me    CO.sub.2 Pr-i                                                                              H         O  H     OMe Me    CH  158-160               I-177                                                                             Me    CO.sub.2 Bu  H         O  H     OMe Me    CH  174-175               I-178                                                                             Me    NO.sub.2     H         O  H     OMe Me    CH  212-214               I-179                                                                             Me    CN           H         O  H     OMe Me    CH  180-181               I-180                                                                             Me    Br           H         O  H     OMe Me    N   166-169               I-181                                                                             Et    Cl           H         O  H     OMe Me    N   141-142               I-182                                                                             Me    OPr          H         O  H     OMe Me    N   210-213               I-183                                                                             Me    OBu          H         O  H     OMe Me    N   184-186               I-184                                                                             Me    OPr-i        H         O  H     OMe Me    N   157-159               I-185                                                                             Me    H            5-OMe     O  H     OMe Me    N                         I-186                                                                             Me    H            5-OEt     O  H     OMe Me    N                         I-187                                                                             Me    H            5-OPr     O  H     OMe Me    N                         I-188                                                                             Me    OCH.sub.2 CF.sub.3                                                                         H         O  H     OMe Me    N                         I-189                                                                             Me    OCH.sub.2 CH.sub.2 OEt                                                                     H         O  H     OMe Me    N                         I-190                                                                             Me    OCH.sub.2 CH.sub.2 OPr-i                                                                   H         O  H     OMe Me    N                         I-191                                                                             Me    OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe Me    N                         I-192                                                                             Me    OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe Me    N                         I-193                                                                             Me    OCH.sub.2 CH.sub.2 NMe.sub.2                                                               H         O  H     OMe Me    N                         I-194                                                                             Me    SEt          H         O  H     OMe Me    N   223-224               I-195                                                                             Me    SPr          H         O  H     OMe Me    N                         I-196                                                                             Me    NMe.sub.2    H         O  H     OMe Me    N                         I-197                                                                             Me    CO.sub.2 Pr-i                                                                              H         O  H     OMe Me    N                         I-198                                                                             Me    CO.sub.2 Bu  H         O  H     OMe Me    N   177-178               I-199                                                                             Me    CN           H         O  H     OMe Me    N   255-258               I-200                                                                             Me    OMe          5-Cl      O  H     Cl  Me    N                         I-201                                                                             Me    Cl           H         O  H     Cl  OMe   CH                        I-202                                                                             Et    Cl           H         O  H     Cl  OMe   CH                        I-203                                                                             Ph    Cl           H         O  H     Cl  OMe   CH                        I-204                                                                             Me    OMe          H         O  H     Cl  OMe   CH  268-269               I-205                                                                             Me    OPr          H         O  H     Cl  OMe   CH  168-169               I-206                                                                             Me    OBu          H         O  H     Cl  OMe   CH  171-173               I-207                                                                             Me    H            5-OMe     O  H     Cl  OMe   CH                        I-208                                                                             Me    OCH.sub.2 CF.sub.3                                                                         H         O  H     Cl  OMe   CH                        I-209                                                                             Me    SPr          H         O  H     Cl  OMe   CH  143-145               I-210                                                                             Me    SBu          H         O  H     Cl  OMe   CH                        I-211                                                                             Me    SPr-i        H         O  H     Cl  OMe   CH  228-230               I-212                                                                             Me    SO.sub.2 Pr-i                                                                              H         O  H     Cl  OMe   CH  143-145               I-213                                                                             Me    NHBn         H         O  H     Cl  OMe   CH                        I-214                                                                             Me    NMe.sub.2    H         O  H     Cl  OMe   CH                        I-215                                                                             Et    Cl           H         O  H     Me  Me    CH                        I-216                                                                             Me    OPr          H         O  H     Me  Me    CH  149-150               I-217                                                                             Me    OBu          H         O  H     Me  Me    CH  146-149               I-218                                                                             Me    OPr-i        H         O  H     Me  Me    CH  174-176               I-219                                                                             Me    NMe.sub.2    H         O  H     Me  Me    CH                        I-220                                                                             Me    OMe          H         O  H     OMe OMe   N                         I-221                                                                             Me    H            5-OEt     O  H     OMe OMe   N                         I-222                                                                             Me    H            5-OPr     O  H     OMe OMe   N                         I-223                                                                             Me    OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe OMe   N                         I-224                                                                             Me    OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe OMe   N                         I-225                                                                             Me    NHMe         H         O  H     OMe Me    CH                        I-226                                                                             Me    NHMe         H         O  H     OMe Me    N                         I-227                                                                             Me    OMe          H         O  H     OMe Me    CH                        I-228                                                                             Me    OMe          5-OMe     O  H     OMe Me    CH                        I-229                                                                             Me    OCHF.sub.2   H         O  H     OMe OMe   CH  198-200               I-230                                                                             Me    OCHF.sub.2   H         O  H     Me  OMe   CH  177-179               I-231                                                                             Me    OCHF.sub.2   H         O  H     Me  OMe   N   165-167               I-232                                                                             Me    OCH.sub.2 CHF.sub.2                                                                        H         O  H     OMe OMe   CH                        I-233                                                                             Me    OCH.sub.2 CHF.sub.2                                                                        H         O  H     Me  OMe   CH                        I-234                                                                             Me    OCH.sub.2 CHF.sub.2                                                                        H         O  H     Me  OMe   N                         I-235                                                                             Me    OCH.sub.2 CH.sub.2 CF.sub.3                                                                H         O  H     OMe OMe   CH                        I-236                                                                             Me    OCH.sub.2 CH.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   CH                        I-237                                                                             Me    OCH.sub.2 CH.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   N                         I-238                                                                             Me    OCH(CF.sub.2 CF.sub.3)Me                                                                   H         O  H     OMe OMe   CH                        I-239                                                                             Me    OCH(CF.sub.2 CF.sub.3)Me                                                                   H         O  H     Me  OMe   CH                        I-240                                                                             Me    OCH(CF.sub.2 CF.sub.3)Me                                                                   H         O  H     Me  OMe   N                         I-241                                                                             Me    OCH.sub.2 CF.sub.2 CHF.sub. 2                                                              H         O  H     OMe OMe   CH                        I-242                                                                             Me    OCH.sub.2 CF.sub.2 CHF.sub.2                                                               H         O  H     Me  OMe   CH                        I-243                                                                             Me    OCH.sub.2 CF.sub.2 CHF.sub.2                                                               H         O  H     Me  OMe   N                         I-244                                                                             Me    OCH.sub.2 CF.sub.2 CF.sub.3                                                                H         O  H     OMe OMe   CH                        I-245                                                                             Me    OCH.sub.2 CF.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   CH                        I-246                                                                             Me    OCH.sub.2 CF.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   N                         I-247                                                                             Me    OCH.sub.2 CHCl.sub.2                                                                       H         O  H     OMe OMe   CH                        I-248                                                                             Me    OCH.sub.2 CHCl.sub.2                                                                       H         O  H     Me  OMe   CH                        I-249                                                                             Me    OCH.sub.2 CHCl.sub.2                                                                       H         O  H     Me  OMe   N                         I-250                                                                             Me    OCF.sub.2 CH.sub.2 Cl                                                                      H         O  H     OMe OMe   CH                        I-251                                                                             Me    OCF.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   CH                        I-252                                                                             Me    OCF.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   N                         I-253                                                                             Me    OCF.sub.2 CHFCl                                                                            H         O  H     OMe OMe   CH                        I-254                                                                             Me    OCF.sub.2 CHFCl                                                                            H         O  H     Me  OMe   CH                        I-255                                                                             Me    OCF.sub.2 CHFCl                                                                            H         O  H     Me  OMe   N                         I-256                                                                             Me    OCF.sub.3    H         O  H     OMe OMe   CH                        I-257                                                                             Me    OCF.sub.3    H         O  H     Me  OMe   CH                        I-258                                                                             Me    OCF.sub.3    H         O  H     Me  OMe   N                         I-259                                                                             Me    OCH.sub.2 CHCHCl                                                                           H         O  H     OMe OMe   CH                        I-260                                                                             Me    OCH.sub.2 CHCHCl                                                                           H         O  H     Me  OMe   CH                        I-261                                                                             Me    OCH.sub.2 CHCHCl                                                                           H         O  H     Me  OMe   N                         I-262                                                                             Me    OCH.sub.2 CHCCl.sub.2                                                                      H         O  H     OMe OMe   CH                        I-263                                                                             Me    OCH.sub.2 CHCCl.sub.2                                                                      H         O  H     Me  OMe   CH                        I-264                                                                             Me    OCH.sub.2 CHCCl.sub.2                                                                      H         O  H     Me  OMe   N                         I-265                                                                             Me    OCH.sub.2 C(Cl)CH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-266                                                                             Me    OCH.sub.2 C(Cl)CH.sub.2                                                                    H         O  H     Me  OMe   CH                        I-267                                                                             Me    OCH.sub.2 C(Cl)CH.sub.2                                                                    H         O  H     Me  OMe   N                         I-268                                                                             Me    OCH.sub.2 C(Me)CH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-269                                                                             Me    OCH.sub.2 C(Me)CH.sub.2                                                                    H         O  H     Me  OMe   CH                        I-270                                                                             Me    OCH.sub.2 C(Me)CH.sub.2                                                                    H         O  H     Me  OMe   N                         I-271                                                                             Me    OCH.sub.2 CHCHMe                                                                           H         O  H     OMe OMe   CH                        I-272                                                                             Me    OCH.sub.2 CHCHMe                                                                           H         O  H     Me  OMe   CH                        I-273                                                                             Me    OCH.sub.2 CH CHMe                                                                          H         O  H     Me  OMe   N                         I-274                                                                             Me    OCH.sub.2 CH.sub.2 N.sub.3                                                                 H         O  H     OMe OMe   CH                        I-275                                                                             Me    OCH.sub.2 CH.sub.2 N.sub.3                                                                 H         O  H     Me  OMe   CH                        I-276                                                                             Me    OCH.sub.2 CH.sub.2 N.sub.3                                                                 H         O  H     Me  OMe   N                         I-277                                                                             Me    OCH.sub.2 OMe                                                                              H         O  H     OMe OMe   CH                        I-278                                                                             Me    OCH.sub.2 OMe                                                                              H         O  H     Me  OMe   CH                        I-279                                                                             Me    OCH.sub.2 OMe                                                                              H         O  H     Me  OMe   N                         I-280                                                                             Me    OCH.sub.2 OEt                                                                              H         O  H     OMe OMe   CH                        I-281                                                                             Me    OCH.sub.2 OEt                                                                              H         O  H     Me  OMe   CH                        I-282                                                                             Me    OCH.sub.2 OEt                                                                              H         O  H     Me  OMe   N                         I-283                                                                             Me    OCH.sub.2 OBn                                                                              H         O  H     OMe OMe   CH                        I-284                                                                             Me    OCH.sub.2 OBn                                                                              H         O  H     Me  OMe   CH                        I-285                                                                             Me    OCH.sub.2 OBn                                                                              H         O  H     Me  OMe   N                         I-286                                                                             Me    OCH.sub.2 OCH.sub.2 CF.sub.3                                                               H         O  H     OMe OMe   CH                        I-287                                                                             Me    OCH.sub.2 OCH.sub.2 CF.sub.3                                                               H         O  H     Me  OMe   CH                        I-288                                                                             Me    OCH.sub.2 OCH.sub.2 CF.sub.3                                                               H         O  H     Me  OMe   N                         I-289                                                                             Me    OCH.sub.2 OBu-t                                                                            H         O  H     OMe OMe   CH                        I-290                                                                             Me    OCH.sub.2 OBu-t                                                                            H         O  H     Me  OMe   CH                        I-291                                                                             Me    OCH.sub.2 OBu-t                                                                            H         O  H     Me  OMe   N                         I-292                                                                             Me    OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                           H         O  H     OMe OMe   CH                        I-293                                                                             Me    OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                           H         O  H     Me  OMe   CH                        I-294                                                                             Me    OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                           H         O  H     Me  OMe   N                         I-295                                                                             Me    OCH.sub.2 CN H         O  H     OMe OMe   CH                        I-296                                                                             Me    OCH.sub.2 CN H         O  H     Me  OMe   CH                        I-297                                                                             Me    OCH.sub.2 CN H         O  H     Me  OMe   N                         I-298                                                                             Me    OCH.sub.2 COOMe                                                                            H         O  H     OMe OMe   CH                        I-299                                                                             Me    OCH.sub.2 COOMe                                                                            H         O  H     Me  OMe   CH                        I-300                                                                             Me    OCH.sub.2 COOMe                                                                            H         O  H     Me  OMe   N                         I-301                                                                             Me    OCH.sub.2 COOPr                                                                            H         O  H     OMe OMe   CH                        I-302                                                                             Me    OCH.sub.2 COOPr                                                                            H         O  H     Me  OMe   CH                        I-303                                                                             Me    OCH.sub.2 COOPr                                                                            H         O  H     Me  OMe   N                         I-304                                                                             Me    OCH.sub.2 COOPr-i                                                                          H         O  H     OMe OMe   CH                        I-305                                                                             Me    OCH.sub.2 COOPr-i                                                                          H         O  H     Me  OMe   CH                        I-306                                                                             Me    OCH.sub.2 COOPr-i                                                                          H         O  H     Me  OMe   N                         I-307                                                                             Me    OCH.sub.2 SMe                                                                              H         O  H     OMe OMe   CH                        I-308                                                                             Me    OCH.sub.2 SMe                                                                              H         O  H     Me  OMe   CH                        I-309                                                                             Me    OCH.sub.2 SMe                                                                              H         O  H     Me  OMe   N                         I-310                                                                             Me    OCH.sub.2 CH.sub.2 SMe                                                                     H         O  H     OMe OMe   CH                        I-311                                                                             Me    OCH.sub.2 CH.sub.2 SMe                                                                     H         O  H     Me  OMe   CH                        I-312                                                                             Me    OCH.sub.2 CH.sub.2 SMe                                                                     H         O  H     Me  OMe   N                         I-313                                                                             Me    SCF.sub.3    H         O  H     OMe OMe   CH                        I-314                                                                             Me    SCF.sub.3    H         O  H     Me  OMe   CH                        I-315                                                                             Me    SCF.sub.3    H         O  H     Me  OMe   N                         I-316                                                                             Me    SCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     OMe OMe   CH                        I-317                                                                             Me    SCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   CH                        I-318                                                                             Me    SCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   N                         I-319                                                                             Me    SCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe OMe   CH                        I-320                                                                             Me    SCH.sub.2 CH.sub.2 F                                                                       H         O  H     Me  OMe   CH                        I-321                                                                             Me    SCH.sub.2 CH.sub.2 F                                                                       H         O  H     Me  OMe   N                         I-322                                                                             Me    SOEt         H         O  H     OMe OMe   CH  185-187               I-323                                                                             Me    SOEt         H         O  H     Me  OMe   CH                        I-324                                                                             Me    SOEt         H         O  H     Me  OMe   N   136-137                                                                       (decomposed)          I-325                                                                             Me    SO.sub.2 NHOEt                                                                             H         O  H     OMe OMe   CH                        I-326                                                                             Me    SO.sub.2 NHOEt                                                                             H         O  H     Me  OMe   CH                        I-327                                                                             Me    SO.sub.2 NHOEt                                                                             H         O  H     Me  OMe   N                         I-328                                                                             Me    SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     OMe OMe   CH                        I-329                                                                             Me    SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     Me  OMe   CH                        I-330                                                                             Me    SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     Me  OMe   N                         I-331                                                                             Me    SO.sub.2 NEt.sub.2                                                                         H         O  H     OMe OMe   CH                        I-332                                                                             Me    SO.sub.2 NEt.sub.2                                                                         H         O  H     Me  OMe   CH                        I-333                                                                             Me    SO.sub.2 NEt.sub.2                                                                         H         O  H     Me  OMe   N                         I-334                                                                             Me    Et           H         O  H     OMe OMe   CH  174-176               I-335                                                                             Me    Et           H         O  H     Me  OMe   CH                        I-336                                                                             Me    Et           H         O  H     Me  OMe   N                         I-337                                                                             Me    Pr           H         O  H     OMe OMe   CH  168-171               I-338                                                                             Me    Pr           H         O  H     Me  OMe   CH                        I-339                                                                             Me    Pr           H         O  H     Me  OMe   N                         I-340                                                                             Me    Pr-i         H         O  H     OMe OMe   CH                        I-341                                                                             Me    Pr-i         H         O  H     Me  OMe   CH                        I-342                                                                             Me    Pr-i         H         O  H     Me  OMe   N                         I-343                                                                             Me    Bu           H         O  H     OMe OMe   CH                        I-344                                                                             Me    Bu           H         O  H     Me  OMe   CH                        I-345                                                                             Me    Bu           H         O  H     Me  OMe   N                         I-346                                                                             Me    Bu-t         H         O  H     OMe OMe   CH                        I-347                                                                             Me    Bu-t         H         O  H     Me  OMe   CH                        I-348                                                                             Me    Bu-t         H         O  H     Me  OMe   N                         I-349                                                                             Me    CH.sub.2 Cl  H         O  H     OMe OMe   CH                        I-350                                                                             Me    CH.sub.2 Cl  H         O  H     Me  OMe   CH                        I-351                                                                             Me    CH.sub.2 Cl  H         O  H     Me  OMe   N                         I-352                                                                             Me    CH.sub.2 F   H         O  H     OMe OMe   CH                        I-353                                                                             Me    CH.sub.2 F   H         O  H     Me  OMe   CH                        I-354                                                                             Me    CH.sub.2 F   H         O  H     Me  OMe   N                         I-355                                                                             Me    CH.sub.2 OMe H         O  H     OMe OMe   CH                        I-356                                                                             Me    CH.sub.2 OMe H         O  H     Me  OMe   CH                        I-357                                                                             Me    CH.sub.2 OMe H         O  H     Me  OMe   N                         I-338                                                                             Me    CH.sub.2 CF.sub.3                                                                          H         O  H     OMe OMe   CH                        I-359                                                                             Me    CH.sub.2 CF.sub.3                                                                          H         O  H     Me  OMe   CH                        I-360                                                                             Me    CH.sub. 2 CF.sub.3                                                                         H         O  H     Me  OMe   N                         I-361                                                                             Me                                                                                   ##STR5##    H         O  H     OMe OMe   CH                        I-362                                                                             Me                                                                                   ##STR6##    H         O  H     Me  OMe   CH                        I-363                                                                             Me                                                                                   ##STR7##    H         O  H     Me  OMe   N                         I-364                                                                             Me    CH.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     OMe OMe   CH                        I-365                                                                             Me    CH.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     Me  OMe   CH                        I-366                                                                             Me    CH.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     Me  OMe   N                         I-367                                                                             Me    CH.sub.2 CHCH.sub.2                                                                        H         O  H     OMe OMe   CH                        I-368                                                                             Me    CH.sub.2 CHCH.sub.2                                                                        H         O  H     Me  OMe   CH                        I-369                                                                             Me    CH.sub.2 CHCH.sub.2                                                                        H         O  H     Me  OMe   N                         I-370                                                                             Me    CH.sub.2 CCH H         O  H     OMe OMe   CH                        I-371                                                                             Me    CH.sub.2 CCH H         O  H     Me  OMe   CH                        I-372                                                                             Me    CH.sub.2 CCH H         O  H     Me  OMe   N                         I-373                                                                             Me    CH.sub.2 COOMe                                                                             H         O  H     OMe OMe   CH                        I-374                                                                             Me    CH.sub.2 COOMe                                                                             H         O  H     Me  OMe   CH                        I-375                                                                             Me    CH.sub.2 COOMe                                                                             H         O  H     Me  OMe   N                         I-376                                                                             Me    CH.sub.2 COOEt                                                                             H         O  H     OMe OMe   CH                        I-377                                                                             Me    CH.sub.2 COOEt                                                                             H         O  H     Me  OMe   CH                        I-378                                                                             Me    CH.sub.2 COOEt                                                                             H         O  H     Me  OMe   N                         I-379                                                                             Me    CH.sub.2 CN  H         O  H     OMe OMe   CH                        I-380                                                                             Me    CH.sub.2 CN  H         O  H     Me  OMe   CH                        I-381                                                                             Me    CH.sub.2 CN  H         O  H     Me  OMe   N                         I-382                                                                             Me    CH.sub.2 CONMe.sub.2                                                                       H         O  H     OMe OMe   CH                        I-383                                                                             Me    CH.sub.2 CONMe.sub.2                                                                       H         O  H     Me  OMe   CH                        I-384                                                                             Me    CH.sub.2 CONMe.sub.2                                                                       H         O  H     Me  OMe   N                         I-385                                                                             Me    CH.sub.2 SO.sub.2 NMe.sub.2                                                                H         O  H     OMe OMe   CH                        I-386                                                                             Me    CH.sub.2 SO.sub.2 NMe.sub.2                                                                H         O  H     Me  OMe   CH                        I-387                                                                             Me    CH.sub.2 SO.sub.2 NMe.sub.2                                                                H         O  H     Me  OMe   N                         I-388                                                                             Me    CH.sub.2 NMe.sub.2                                                                         H         O  H     OMe OMe   CH                        I-389                                                                             Me    CH.sub.2 NMe.sub.2                                                                         H         O  H     Me  OMe   CH                        I-390                                                                             Me    CH.sub. 2 NMe.sub.2                                                                        H         O  H     Me  OMe   N                         I-391                                                                             Me    CHCH.sub.2   H         O  H     OMe OMe   CH                        I-392                                                                             Me    CHCH.sub.2   H         O  H     Me  OMe   CH                        I-393                                                                             Me    CHCH.sub.2   H         O  H     Me  OMe   N                         I-394                                                                             Me    CHCHMe       H         O  B     OMe OMe   CH                        I-395                                                                             Me    CHCHMe       H         O  H     Me  OMe   CH                        I-396                                                                             Me    CHCHMe       H         O  H     Me  OMe   N                         I-397                                                                             Me    CCH          H         O  H     OMe OMe   CH                        I-398                                                                             Me    CCH          H         O  H     Me  OMe   CH                        I-399                                                                             Me    CCH          H         O  H     Me  OMe   N                         I-400                                                                             Me    CCMe         H         O  H     OMe OMe   CH                        I-401                                                                             Me    CCMe         H         O  H     Me  OMe   CH                        I-402                                                                             Me    CCMe         H         O  H     Me  OMe   N                         I-403                                                                             Me    CHCHCOOMe    H         O  H     OMe OMe   CH                        I-404                                                                             Me    CHCHCOOMe    H         O  H     Me  OMe   CH                        I-405                                                                             Me    CHCHCOOMe    H         O  H     Me  OMe   N                         I-406                                                                             Me    CH(Me)COMe   H         O  H     OMe OMe   CH                        I-407                                                                             Me    CH(Me)COMe   H         O  H     Me  OMe   CH                        I-408                                                                             Me    CH(Me)COMe   H         O  H     Me  OMe   N                         I-409                                                                             Me    CH(Me)COEt   H         O  H     OMe OMe   CH                        I-410                                                                             Me    CH(Me)COEt   H         O  H     Me  OMe   CH                        I-411                                                                             Me    CH(Me)COEt   H         O  H     Me  OMe   N                         I-412                                                                             Me    CH(Et)COMe   H         O  H     OMe OMe   CH                        I-413                                                                             Me    CH(Et)COMe   H         O  H     Me  OMe   CH                        I-414                                                                             Me    CH(Et)COMe   H         O  H     Me  OMe   N                         I-415                                                                             Me    CH(Et)COEt   H         O  H     OMe OMe   CH                        I-416                                                                             Me    CH(Et)COEt   H         O  H     Me  OMe   CH                        I-417                                                                             Me    CH(Et)COEt   H         O  H     Me  OMe   N                         I-418                                                                             Me                                                                                   ##STR8##    H         O  H     OMe OMe   CH                        I-419                                                                             Me                                                                                   ##STR9##    H         O  H     Me  OMe   CH                        I-420                                                                             Me                                                                                   ##STR10##   H         O  H     Me  OMe   N                         I-421                                                                             Me    COPr         H         O  H     OMe OMe   CH                        I-422                                                                             Me    COPr         H         O  H     Me  OMe   CH                        I-423                                                                             Me    COPr         H         O  H     Me  OMe   N                         I-424                                                                             Me    COPr-i       H         O  H     OMe OMe   CH                        I-425                                                                             Me    COPr-i       H         O  H     Me  OMe   CH                        I-426                                                                             Me    COPr-i       H         O  H     Me  OMe   N                         I-427                                                                             Me    CHNOMe       H         O  H     OMe OMe   CH                        I-428                                                                             Me    CHNOMe       H         O  H     Me  OMe   CH                        I-429                                                                             Me    CHNOMe       H         O  H     Me  OMe   N                         I-430                                                                             Me    CHNOEt       H         O  H     OMe OMe   CH                        I-431                                                                             Me    CHNOEt       H         O  H     Me  OMe   CH                        I-432                                                                             Me    CHNOEt       H         O  H     Me  OMe   N                         I-433                                                                             Me    C(Me)NOMe    H         O  H     OMe OMe   CH                        I-434                                                                             Me    C(Me)NOMe    H         O  H     Me  OMe   CH                        I-435                                                                             Me    C(Me)NOMe    H         O  H     Me  OMe   N                         I-436                                                                             Me    C(Me)NOEt    H         O  H     OMe OMe   CH                        I-437                                                                             Me    C(Me)NOEt    H         O  H     Me  OMe   CH                        I-438                                                                             Me    C(Me)NOEt    H         O  H     Me  OMe   N                         I-439                                                                             Me    C(Me)NOPr    H         O  H     OMe OMe   CH                        I-440                                                                             Me    C(Me)NOPr    H         O  H     Me  OMe   CH                        I-441                                                                             Me    C(Me)NOPr    H         O  H     Me  OMe   N                         I-442                                                                             Me    C(Me)NOCH.sub.2 CH.sub.2 Cl                                                                H         O  H     OMe OMe   CH                        I-443                                                                             Me    C(Me) NOCH.sub.2 CH.sub.2 Cl                                                               H         O  H     Me  OMe   CH                        I-444                                                                             Me    C(Me)NOCH.sub.2 CH.sub.2 Cl                                                                H         O  H     Me  OMe   N                         I-445                                                                             Me    C(Me)NOCH.sub.2 CH.sub.2 F                                                                 H         O  H     OMe OMe   CH                        I-446                                                                             Me    C(Me)NOCH.sub.2 CH.sub.2 F                                                                 H         O  H     Me  OMe   CH                        I-447                                                                             Me    C(Me)NOCH.sub.2 CH.sub.2 F                                                                 H         O  H     Me  OMe   N                         I-448                                                                             Me    NHEt         H         O  H     OMe OMe   CH                        I-449                                                                             Me    NHEt         H         O  H     Me  OMe   CH                        I-450                                                                             Me    NHEt         H         O  H     Me  OMe   N                         I-451                                                                             Me    NHPr         H         O  H     OMe OMe   CH                        I-452                                                                             Me    NHPr         H         O  H     Me  OMe   CH                        I-453                                                                             Me    NHPr         H         O  H     Me  OMe   N                         I-454                                                                             Me    NHCOOMe      H         O  H     OMe OMe   CH                        I-455                                                                             Me    NHCOOMe      H         O  H     Me  OMe   CH                        I-456                                                                             Me    NHCOOMe      H         O  H     Me  OMe   N                         I-457                                                                             Me    NHCOOEt      H         O  H     OMe OMe   CH                        I-458                                                                             Me    NHCOOEt      H         O  H     Me  OMe   CH                        I-459                                                                             Me    NHCOOEt      H         O  H     Me  OMe   N                         I-460                                                                             Me    NHCOOPh      H         O  H     OMe OMe   CH                        I-461                                                                             Me    NHCOOPh      H         O  H     Me  OMe   CH                        I-462                                                                             Me    NHCOOPh      H         O  H     Me  OMe   N                         I-463                                                                             Me    N(Me)SO.sub.2 Me                                                                           H         O  H     OMe OMe   CH                        I-464                                                                             Me    N(Me)SO.sub.2 Me                                                                           H         O  H     Me  OMe   CH                        I-465                                                                             Me    N(Me)SO.sub.2 Me                                                                           H         O  H     Me  OMe   N                         I-466                                                                             Me    N(Et)SO.sub.2 Me                                                                           H         O  H     OMe OMe   CH                        I-467                                                                             Me    N(Et)SO.sub.2 Me                                                                           H         O  H     Me  OMe   CH                        I-468                                                                             Me    N(Et)SO.sub.2 Me                                                                           H         O  H     Me  OMe   N                         I-469                                                                             Me    N(Me)SO.sub.2 Et                                                                           H         O  H     OMe OMe   CH                        I-470                                                                             Me    N(Me)SO.sub.2 Et                                                                           H         O  H     Me  OMe   CH                        I-471                                                                             Me    N(Me)SO.sub.2 Et                                                                           H         O  H     Me  OMe   N                         I-472                                                                             Me    N(Et)SO.sub.2 Et                                                                           H         O  H     OMe OMe   CH                        I-473                                                                             Me    N(Et)SO.sub.2 Et                                                                           H         O  H     Me  OMe   CH                        I-474                                                                             Me    N(Et)SO.sub.2 Et                                                                           H         O  H     Me  OMe   N                         I-475                                                                             Me    NHCOEt       H         O  H     OMe OMe   CH                        I-476                                                                             Me    NHCOEt       H         O  H     Me  OMe   CH                        I-477                                                                             Me    NHCOEt       H         O  H     Me  OMe   N                         I-478                                                                             Me    NHCOCF.sub.3 H         O  H     OMe OMe   CH                        I-479                                                                             Me    NHCOCF.sub.3 H         O  H     Me  OMe   CH                        I-480                                                                             Me    NHCOCF.sub.3 H         O  H     Me  OMe   N                         I-481                                                                             Me    NCHMe        H         O  H     OMe OMe   CH                        I-482                                                                             Me    NCHMe        H         O  H     Me  OMe   CH                        I-483                                                                             Me    NCHMe        H         O  H     Me  OMe   N                         I-484                                                                             Me    NCHPh        H         O  H     OMe OMe   CH                        I-485                                                                             Me    NCHPh        H         O  H     Me  OMe   CH                        I-486                                                                             Me    NCHPh        H         O  H     Me  OMe   N                         I-487                                                                             Me    N.sub.3      H         O  H     OMe OMe   CH                        I-488                                                                             Me    N.sub.3      H         O  H     Me  OMe   CH                        I-489                                                                             Me    N.sub.3      H         O  H     Me  OMe   N                         I-490                                                                             Me    I            H         O  H     OMe OMe   CH                        I-491                                                                             Me    I            H         O  H     Me  OMe   CH                        I-492                                                                             Me    I            H         O  H     Me  OMe   N                         I-493                                                                             Me    OCOEt        H         O  H     OMe OMe   CH                        I-494                                                                             Me    OCOEt        H         O  H     Me  OMe   CH                        I-495                                                                             Me    OCOEt        H         O  H     Me  OMe   N                         I-496                                                                             Me    OCOPr        H         O  H     OMe OMe   CH                        I-497                                                                             Me    OCOPr        H         O  H     Me  OMe   CH                        I-498                                                                             Me    OCOPr        H         O  H     Me  OMe   N                         I-499                                                                             Me    OCOPh        H         O  H     OMe OMe   CH                        I-500                                                                             Me    OCOPh        H         O  H     Me  OMe   CH                        I-501                                                                             Me    OCOPh        H         O  H     Me  OMe   N                         I-502                                                                             Me    OCONMe.sub.2 H         O  H     OMe OMe   CH                        I-503                                                                             Me    OCONMe.sub.2 H         O  H     Me  OMe   CH                        I-504                                                                             Me    OCONMe.sub.2 H         O  H     Me  OMe   N                         I-505                                                                             Me    Cl           H         O  H     CF.sub.3                                                                          OMe   CH                        I-506                                                                             Me    OPr-i        H         O  H     Cl  OMe   CH  163-165               I-507                                                                             Me    SEt          H         O  H     Me  OMe   CH  225-227               I-508                                                                             Me    SEt          H         O  H     Cl  OMe   CH  185-187               I-509                                                                             Me    SEt          H         O  H     Me  Me    CH  220-222               I-510                                                                             Me    SEt          H         O  H     OMe OMe   N   173-175               I-511                                                                             Me    SBu          H         O  H     OMe Me    CH  157-160               I-512                                                                             Me    SBu          H         O  H     OMe Me    N   155-157               I-513                                                                             Me    SPr-i        H         O  H     OMe Me    CH  185-187               I-514                                                                             Me    SPr-i        H         O  H     OMe Me    N   228-229               I-515                                                                             Me    SOEt         H         O  H     OMe OMe   N   180-182               I-516                                                                             Me    SO.sub.2 Et  H         O  H     OMe Me    CH  270-272               I-517                                                                             Me    SO.sub.2 Et  H         O  H     OMe Me    N   165-168               I-518                                                                             Me    SO.sub.2 Et  H         O  H     OMe Cl    CH  272-275               I-519                                                                             Me    SO.sub.2 Pr  H         O  H     OMe Me    CH  265-267               I-520                                                                             Me    SO.sub.2 Pr  H         O  H     OMe Me    N   132-135               I-521                                                                             Me    SO.sub.2 Pr  H         O  H     OMe Cl    CH  142-145               I-522                                                                             Me    SO.sub.2 Bu  H         O  H     OMe Me    CH  243-246               I-523                                                                             Me    SO.sub.2 Bu  H         O  H     OMe Me    N   241-243               I-524                                                                             Me    SO.sub.2 Bu  H         O  H     OMe Cl    CH  245-247               I-525                                                                             Me    SO.sub.2 Pr-i                                                                              H         O  H     OMe Me    CH  135-139               I-526                                                                             Me    SO.sub.2 Pr-i                                                                              H         O  H     OMe Me    N   281-282               I-527                                                                             Me    COOPr        H         O  H     OMe Me    N   187-189               I-528                                                                             Me    NO.sub.2     H         O  H     OMe Cl    CH  204-206               I-529                                                                             Me    CONMe.sub.2  H         O  H     OMe Me    CH  161-164               I-530                                                                             Me    Br           H         O  H     OMe Cl    CH  276-279               I-531                                                                             Me                                                                                   ##STR11##   H         O  H     OMe OMe   CH                        I-532                                                                             Me    OCH.sub.2Bu-t                                                                              H         O  H     OMe OMe   CH                        I-533                                                                             Me    OCH.sub.2Bu-t                                                                              H         O  H     Me  OMe   CH                        I-534                                                                             Me    OCH.sub.2 CHCMe.sub.2                                                                      H         O  H     OMe OMe   CH                        I-535                                                                             Me    OCH.sub.2 CH.sub.2 CH.sub.2 F                                                              H         O  H     OMe OMe   CH                        I-536                                                                             Me    OCH.sub.2 CH.sub.2 CH.sub.2 F                                                              H         O  H     Me  OMe   CH                        I-537                                                                             Me    OCH.sub.2 CH.sub.2 CH.sub.2 F                                                              H         O  H     Me  OMe   N                         I-538                                                                             Me    CH.sub.2 CH.sub.2 3                                                                        H         O  H     OMe OMe   CH                        I-539                                                                             Me                                                                                   ##STR12##   H         O  H     OMe OMe   CH                        I-540                                                                             Me    COCF.sub.3   H         O  H     OMe OMe   CH                        I-541                                                                             Me    COOCH.sub.2 CHCHCl                                                                         H         O  H     OMe OMe   CH                        I-542                                                                             Me    SO.sub.2 CF.sub.3                                                                          H         O  H     OMe OMe   CH                        I-543                                                                             Me    OCOCF.sub.3  H         O  H     OMe OMe   CH                        I-544                                                                             Me    OCH.sub.2 OPh                                                                              H         O  H     OMe OMe   CH                        I-545                                                                             Me    CHNOH        H         O  H     OMe OMe   CH                        I-546                                                                             Me    CHNOCH.sub.2 CHCH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-547                                                                             Me    CHNOCH.sub.2 CCH                                                                           H         O  H     OMe OMe   CH                        I-548                                                                             Me    C(Me)NOBn    H         O  H     OMe OMe   CH                        I-549                                                                             Me    C(Me)NOPh    H         O  H     OMe OMe   CH                        I-550                                                                             Me    C(Bn)NOMe    H         O  H     OMe OMe   CH                        I-551                                                                             Me    C(Ph)NOMe    H         O  H     OMe OMe   CH                        I-552                                                                             Me    C(CF.sub.3)NOMe                                                                            H         O  H     OMe OMe   CH                        I-553                                                                             Me    COOCH.sub.2 CH.sub.2 Cl                                                                    H         O  H     OMe OMe   CH                        I-554                                                                             Me    COOCH.sub.2 CF.sub.3                                                                       H         O  H     OMe OMe   CH                        I-555                                                                             Me    Cl           5-Cl      O  H     OMe Me    N   182-184               I-556                                                                             Me    Cl           5-OMe     O  H     OMe OMe   CH                        I-557                                                                             Me    Cl           5-F       O  H     OMe OMe   CH                        I-558                                                                             Me    F            5-Cl      O  H     OMe OMe   CH                        I-559                                                                             Me    F            5-F       O  H     OMe OMe   CH                        I-560                                                                             Me    COOMe        5-Cl      O  H     OMe OMe   CH                        I-561                                                                             Me    COOEt        5-Cl      O  H     OMe OMe   CH                        I-562                                                                             Me    COOPr        5-Cl      O  H     OMe OMe   CH                        I-563                                                                             Me    COOPr-i      5-Cl      O  H     OMe OMe   CH                        I-564                                                                             Me    OMe          5-COOMe   O  H     OMe OMe   CH                        I-565                                                                             Me    COOMe        5-OMe     O  H     OMe OMe   CH                        I-566                                                                             Me    H            5-CN      O  H     OMe OMe   CH                        I-567                                                                             Me    H            5-CF.sub.3                                                                              O  H     OMe OMe   CH                        I-568                                                                             Me    H            5-COOMe   O  H     OMe OMe   CH  235-236               I-569                                                                             Me    H            5-COOEt   O  H     OMe OMe   CH                        I-570                                                                             Me    H            5-COOPr   O  H     OMe OMe   CH                        I-571                                                                             Me    H            5-COOPr-i O  H     OMe OMe   CH                        I-572                                                                             Me    H            5-COOCH.sub. 2 CH.sub.2 Cl                                                              O  H     OMe OMe   CH                        I-573                                                                             Me    H            5-COOCH.sub.2 CH.sub.2 F                                                                O  H     OMe OMe   CH                        I-574                                                                             Me    H            5-COOCH.sub.2 CF.sub.3                                                                  O  H     OMe OMe   CH                        I-575                                                                             Me    H            5-COOCH.sub.2 OMe                                                                       O  H     OMe OMe   CH                        I-576                                                                             Me    H            5-CONMe.sub.2                                                                           O  H     OMe OMe   CH                        I-577                                                                             Me    H            5-OCH.sub.2 CH.sub.2 F                                                                  O  H     OMe OMe   CH                        I-578                                                                             Me    H            5-OCH.sub.2 CF.sub.2                                                                    O  H     OMe OMe   CH                        I-579                                                                             Me    H            5-OCH.sub.2 CF.sub.3                                                                    O  H     OMe OMe   CH                        I-580                                                                             Me    H            5-OCH.sub.2 CH.sub.2 CH.sub.2 F                                                         O  H     OMe OMe   CH                        I-581                                                                             Me    H            5-OCH.sub.2 CHCH.sub.2                                                                  O  H     OMe OMe   CH                        I-582                                                                             Me    H            5-OCH.sub.2 CCH                                                                         O  H     OMe OMe   CH                        I-583                                                                             Me    H            5-NO.sub.2                                                                              O  H     OMe OMe   CH                        I-584                                                                             Me    H            5-SMe     O  H     OMe OMe   CH                        I-585                                                                             Me    H            5-SEt     O  H     OMe OMe   CH                        I-586                                                                             Me    H            5-SPr     O  H     OMe OMe   CH                        I-587                                                                             Me    H            5-SPr-i   O  H     OMe OMe   CH                        I-588                                                                             Me    H            5-SO.sub.2 Et                                                                           O  H     OMe OMe   CH                        I-589                                                                             Me    H            5-SO.sub.2 Pr                                                                           O  H     OMe OMe   CH                        I-590                                                                             Me    H            5-SO.sub.2 Pr-i                                                                         O  H     OMe OMe   CH                        I-591                                                                             Me    H            5-SOEt    O  H     OMe OMe   CH                        I-592                                                                             Me    H            5-Me      O  H     OMe OMe   CH                        I-593                                                                             Me    H            5-Et      O  H     OMe OMe   CH                        I-594                                                                             Me    H            5-Pr      O  H     OMe OMe   CH                        I-595                                                                             Me    H            5-SO.sub.2 NMe.sub.2                                                                    O  H     OMe OMe   CH                        I-596                                                                             Me    H            5-OCF.sub.3                                                                             O  H     OMe OMe   CH                        I-597                                                                             Me    H            5-CH.sub.2 CF.sub.3                                                                     O  H     OMe OMe   CH                        I-598                                                                             Me    H            5-CH.sub.2 CHCH.sub.2                                                                   O  H     OMe OMe   CH                        I-599                                                                             Me    H            5-COOMe   O  H     OMe Me    CH  134-135               I-600                                                                             Me    H            5-COOMe   O  H     OMe Me    N   143-144               I-601                                                                             Me    H            5-COOMe   O  H     OMe OMe   N   148-150               I-602                                                                             Me                                                                                   ##STR13##   H         O  H     OMe OMe   CH                        I-603                                                                             Me                                                                                   ##STR14##   H         O  H     Me  OMe   CH                        I-604                                                                             Me                                                                                   ##STR15##   H         O  H     Me  OMe   N                         I-605                                                                             Me                                                                                   ##STR16##   H         O  H     OMe OMe   CH                        I-606                                                                             Me                                                                                   ##STR17##   H         O  H     Me  OMe   CH                        I-607                                                                             Me                                                                                   ##STR18##   H         O  H     Me  OMe   N                         I-608                                                                             Me                                                                                   ##STR19##   H         O  H     OMe OMe   CH                        I-609                                                                             Me                                                                                   ##STR20##   H         O  H     Me  OMe   CH                        I-610                                                                             Me                                                                                   ##STR21##   H         O  H     Me  OMe   N                         I-611                                                                             Me    OC.sub.2 H.sub.4 O*    O  H     OMe OMe   CH                        I-612                                                                             Me    OC.sub.2 H.sub.4 O*    O  H     Me  OMe   CH                        I-613                                                                             Me    OC.sub.2 H.sub.4 O*    O  H     Me  OMe   N                         I-614                                                                             Me    SC.sub.2 H.sub.4 S*    O  H     OMe OMe   CH                        I-615                                                                             Me    SC.sub.2 H.sub.4 S*    O  H     Me  OMe   CH                        I-616                                                                             Me    SC.sub.2 H.sub.4 S*    O  H     Me  OMe   N                         I-617                                                                             Me    OCH.sub.2 O*           O  H     OMe OMe   CH                        I-618                                                                              ##STR22##  Cl     H         O  H     OMe OMe   CH                        I-619                                                                              ##STR23##  Cl     H         O  H     OMe OMe   CH                        I-620                                                                              ##STR24##  Cl     H         O  H     OMe OMe   CH                        I-621                                                                             COMe        Cl     H         O  H     OMe OMe   CH                        I-622                                                                             COEt        Cl     H         O  H     OMe OMe   CH                        I-623                                                                             COPr        Cl     H         O  H     OMe OMe   CH                        I-624                                                                             COPr-i      Cl     H         O  H     OMe OMe   CH                        I-625                                                                             COPh        Cl     H         O  H     OMe OMe   CH                        I-626                                                                             SO.sub.2 Me Cl     H         O  H     OMe OMe   CH                        I-627                                                                             SO.sub.2 Et Cl     H         O  H     OMe OMe   CH                        I-628                                                                             SO.sub.2 Ph Cl     H         O  H     OMe OMe   CH                        I-629                                                                             COOMe       Cl     H         O  H     OMe OMe   CH                        I-630                                                                             COOEt       Cl     H         O  H     OMe OMe   CH                        I-631                                                                             COOPh       Cl     H         O  H     OMe OMe   CH                        I-632                                                                             CONMe.sub.2 Cl     H         O  H     OMe OMe   CH                        I-633                                                                             SO.sub.2 NMe.sub.2                                                                        Cl     H         O  H     OMe OMe   CH                        I-634                                                                             Ph          Cl     H         O  H     Me  OMe   N                         I-635                                                                             CH.sub.2 OMe                                                                              Cl     H         O  H     OMe OMe   CH                        I-636                                                                             CH.sub.2 OBn                                                                              Cl     H         O  H     OMe OMe   CH                        I-637                                                                             CH.sub.2 CH.sub.2 F                                                                       Cl     H         O  H     OMe OMe   CH                        I-638                                                                             CH.sub.2 CH.sub.2 Cl                                                                      Cl     H         O  H     OMe OMe   CH                        I-639                                                                             CF.sub.3    Cl     H         O  H     OMe OMe   CH                        I-640                                                                             CH.sub.2 F  Cl     H         O  H     OMe OMe   CH                        I-641                                                                             CH.sub.2 CHCH.sub.2                                                                       OMe    H         O  H     OMe OMe   CH  221-223               I-642                                                                             COCF.sub.3  Cl     H         O  H     OMe OMe   CH                        I-643                                                                              ##STR25##  Cl     H         O  H     OMe OMe   CH                        I-644                                                                             H     Bn           H         O  H     OMe OMe   CH                        I-645                                                                             H     Br           H         O  H     OMe Me    CH  183-184               I-646                                                                             H     Br           H         O  H     OMe Me    N   154-155               I-647                                                                             N     Br           H         O  H     OMe OMe   CH                        I-648                                                                             H     Bu           H         O  H     Me  OMe   CH                        I-649                                                                             H     Bu           H         O  H     Me  OMe   N                         I-650                                                                             H     Bu           H         O  H     OMe OMe   CH                        I-651                                                                             H     Bu-t         H         O  H     Me  OMe   CH                        I-652                                                                             H     Bu-t         H         O  H     Me  OMe   N                         I-653                                                                             H     Bu-t         H         O  H     OMe OMe   CH                        I-654                                                                             H     C(Me)NOCH.sub.2 CH.sub.2 Cl                                                                H         O  H     Me  OMe   CH                        I-655                                                                             H     C(Me)NOCH.sub.2 CH.sub.2 Cl                                                                H         O  H     Me  OMe   N                         I-656                                                                             H     C(Me)NOCH.sub.2 CH.sub.2 Cl                                                                H         O  H     OMe OMe   CH                        I-657                                                                             H     C(Me)NOCH.sub.2 CH.sub.2 F                                                                 H         O  H     Me  OMe   CH                        I-658                                                                             H     C(Me)NOCH.sub.2 CH.sub.2 F                                                                 H         O  H     Me  OMe   N                         I-659                                                                             H     C(Me)NOCH.sub.2 CH.sub.2 F                                                                 H         O  H     OMe OMe   CH                        I-660                                                                             H     C(Me)NOEt    H         O  H     Me  OMe   CH                        I-661                                                                             H     C(Me)NOEt    H         O  H     Me  OMe   N                         I-662                                                                             H     C(Me)NOEt    H         O  H     OMe OMe   CH                        I-663                                                                             H     C(Me)NOMe    H         O  H     Me  OMe   CH                        I-664                                                                             H     C(Me)NOMe    H         O  H     Me  OMe   N                         I-665                                                                             H     C(Me)NOMe    H         O  H     OMe OMe   CH                        I-666                                                                             H     C(Me)NOPr    H         O  H     Me  OMe   CH                        I-667                                                                             H     C(Me) NOPr   H         O  H     Me  OMe   N                         I-668                                                                             H     C(Me)NOPr    H         O  H     OMe OMe   CH                        I-669                                                                             H     CCH          H         O  H     Me  OMe   CH                        I-670                                                                             H     CCH          H         O  H     Me  OMe   N                         I-671                                                                             H     CCH          H         O  H     OMe OMe   CH                        I-672                                                                             H     CCMe         H         O  H     Me  OMe   CH                        I-673                                                                             H     CCMe         H         O  H     Me  OMe   N                         I-674                                                                             H     CCMe         H         O  H     OMe OMe   CH                        I-675                                                                             H     CF.sub.3     H         O  H     OMe OMe   CH                        I-676                                                                             H     CH(Et)COEt   H         O  H     Me  OMe   CH                        I-677                                                                             H     CH(Et)COEt   H         O  H     Me  OMe   N                         I-678                                                                             H     CH(Et)COEt   H         O  H     OMe OMe   CH                        I-679                                                                             H     CH(Et)COMe   H         O  H     Me  OMe   CH                        I-680                                                                             H     CH(Et)COMe   H         O  H     Me  OMe   N                         I-681                                                                             H     CH(Et)COMe   H         O  H     OMe OMe   CH                        I-682                                                                             H     CH(Me)COEt   H         O  H     Me  OMe   CH                        I-683                                                                             H     CH(Me)COEt   H         O  H     Me  OMe   N                         I-684                                                                             H     CH(Me)COEt   H         O  H     OMe OMe   CH                        I-685                                                                             H     CH(Me)COMe   H         O  H     Me  OMe   CH                        I-686                                                                             H     CH(Me)COMe   H         O  H     Me  OMe   N                         I-687                                                                             H     CH(Me)COMe   H         O  H     OMe OMe   CH                        I-688                                                                             H     CHCHCOOMe    H         O  H     Me  OMe   CH                        I-689                                                                             H     CHCHCOOMe    H         O  H     Me  OMe   N                         I-690                                                                             H     CHCHCOOMe    H         O  H     OMe OMe   CH                        I-691                                                                             H     CHCH.sub.2   H         O  H     Me  OMe   CH                        I-692                                                                             H     CHCH.sub.2   H         O  H     Me  OMe   N                         I-693                                                                             H     CHCH.sub.2   H         O  N     OMe OMe   CH                        I-694                                                                             H     CHCHMe       H         O  H     Me  OMe   CH                        I-695                                                                             H     CHCHMe       H         O  H     Me  OMe   N                         I-696                                                                             H     CHCHMe       H         O  H     OMe OMe   CH                        I-697                                                                             H     CHNOEt       H         O  H     Me  OMe   CH                        I-698                                                                             H     CHNOEt       H         O  H     Me  OMe   N                         I-699                                                                             H     CHNOEt       H         O  H     OMe OMe   CH                        I-700                                                                             H     CHNOMe       H         O  H     Me  OMe   CH                        I-701                                                                             H     CHNOMe       H         O  H     Me  OMe   N                         I-702                                                                             H     CHNOMe       H         O  H     OMe OMe   CH                        I-703                                                                             H     CH.sub.2 CCH H         O  H     Me  OMe   CH                        I-704                                                                             H     CH.sub.2 CCH H         O  H     Me  OMe   N                         I-705                                                                             H     CH.sub.2 CCH H         O  H     OMe OMe   CH                        I-706                                                                             H     CF.sub.2 CF.sub.3                                                                          H         O  H     Me  OMe   CH                        I-707                                                                             H     CH.sub.2 CF.sub.3                                                                          H         O  H     Me  OMe   N                         I-708                                                                             H     CH.sub.2 CF.sub.3                                                                          H         O  H     OMe OMe   CH                        I-709                                                                             H     CH.sub.2 CHCH.sub.2                                                                        H         O  H     Me  OMe   CH                        I-710                                                                             H     CH.sub.2 CHCH.sub.2                                                                        H         O  H     Me  OMe   N                         I-711                                                                             H     CH.sub.2 CHCH.sub.2                                                                        H         O  H     OMe OMe   CH                        I-712                                                                             H     CH.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     Me  OMe   CH                        I-713                                                                             H     CH.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     Me  OMe   N                         I-714                                                                             H     CH.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     OMe OMe   CH                        I-715                                                                             H     CH.sub.2 CN  H         O  H     Me  OMe   CH                        I-716                                                                             H     CH.sub.2 CN  H         O  H     Me  OMe   N                         I-717                                                                             H     CH.sub.2 CN  H         O  H     OMe OMe   CH                        I-718                                                                             H     CH.sub.2 CONMe.sub.2                                                                       H         O  H     Me  OMe   CH                        I-719                                                                             H     CH.sub.2 CONMe.sub.2                                                                       H         O  H     Me  OMe   N                         I-720                                                                             H     CH.sub.2 CONMe.sub.2                                                                       H         O  H     OMe OMe   CH                        I-721                                                                             H     CH.sub.2 COOEt                                                                             H         O  H     Me  OMe   CH                        I-722                                                                             H     CH.sub.2 COOEt                                                                             H         O  H     Me  OMe   N                         I-723                                                                             H     CH.sub.2 COOEt                                                                             H         O  H     OMe OMe   CH                        I-724                                                                             H     CH.sub.2 COOMe                                                                             H         O  H     Me  OMe   CH                        I-725                                                                             H     CH.sub.2 COOMe                                                                             H         O  H     Me  OMe   N                         I-726                                                                             H     CH.sub.2 COOMe                                                                             H         O  H     OMe OMe   CH                        I-727                                                                             H     CH.sub.2 Cl  H         O  H     Me  OMe   CH                        I-728                                                                             H     CH.sub.2 Cl  H         O  H     Me  OMe   N                         I-729                                                                             H     CH.sub.2 Cl  H         O  H     OMe OMe   CH                        I-730                                                                             H     CH.sub.2 F   H         O  H     Me  OMe   CH                        I-731                                                                             H     CH.sub.2 F   H         O  H     Me  OMe   N                         I-732                                                                             H     CH.sub.2 F   H         O  H     OMe OMe   CH                        I-733                                                                             H     CH.sub.2 NMe.sub. 2                                                                        H         O  H     Me  OMe   CH                        I-734                                                                             H     CH.sub.2 NMe.sub.2                                                                         H         O  H     Me  OMe   N                         I-735                                                                             H     CH.sub.2 NMe.sub.2                                                                         H         O  H     OMe OMe   CH                        I-736                                                                             H     CH.sub.2 OMe H         O  H     Me  OMe   CH                        I-737                                                                             H     CH.sub.2 OMe H         O  H     Me  OMe   N                         I-738                                                                             H     CH.sub.2 OMe H         O  H     OMe OMe   CH                        I-739                                                                             H     CH.sub.2 SO.sub.2 NMe.sub.2                                                                H         O  H     Me  OMe   CH                        I-740                                                                             H     CH.sub.2 SO.sub.2 NMe.sub.2                                                                H         O  H     Me  OMe   N                         I-741                                                                             H     CH.sub.2 SO.sub.2 NMe.sub.2                                                                H         O  H     OMe OMe   CH                        I-742                                                                             H     CN           H         O  H     OMe Me    CH                        I-743                                                                             H     CN           H         O  H     OMe Me    N                         I-744                                                                             H     CN           H         O  H     OMe OMe   CH                        I-745                                                                             H                                                                                    ##STR26##   H         O  H     Me  OMe   CH                        I-746                                                                             H                                                                                    ##STR27##   H         O  H     Me  OMe   N                         I-747                                                                             H                                                                                    ##STR28##   H         O  H     OMe OMe   CH                        I-748                                                                             H     CO.sub.2 Bn  H         O  H     OMe OMe   CH                        I-749                                                                             H     CO.sub.2 Bu  H         O  H     OMe Me    CH                        I-750                                                                             H     CO.sub.2 Bu  H         O  H     OMe Me    N                         I-751                                                                             H     CO.sub.2 Bu  H         O  H     OMe OMe   CH                        I-752                                                                             H     CO.sub.2 CH.sub.2 CCH                                                                      H         O  H     OMe OMe   CH                        I-753                                                                             H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     OMe OMe   CH                        I-754                                                                             H     CO.sub.2 CH.sub.2 CH.sub.2 F                                                               H         O  H     OMe OMe   CH                        I-755                                                                             H     CO.sub.2 Et  H         O  H     OCHF.sub.2                                                                        OCHF.sub.2                                                                          CH                        I-756                                                                             H     CO.sub.2 Et  H         O  H     OMe Me    N                         I-757                                                                             H     CO.sub.2 Et  H         S  H     OMe OMe   CH                        I-758                                                                             H     CO.sub.2 H   H         O  H     OMe OMe   CH                        I-759                                                                             H     CO.sub.2 Me  5-F       O  H     OMe OMe   CH                        I-760                                                                             H     CO.sub.2 Me  H         O  H     OCHF.sub.2                                                                        OCHF.sub.2                                                                          CH                        I-761                                                                             H     CO.sub.2 Me  H         O  H     OMe Me    CH  202-205               I-762                                                                             H     CO.sub.2 Me  H         O  H     OMe Me    N   169-170               I-763                                                                             H     CO.sub.2 Me  H         O  H     OMe OCHF.sub.2                                                                          CH                        I-764                                                                             H     CO.sub.2 Me  H         O  Me    OMe OMe   CH                        I-765                                                                             H     CO.sub.2 Me  H         S  H     OMe OMe   CH                        I-766                                                                             H     CO.sub.2 Pen H         O  H     OMe OMe   CH                        I-767                                                                             H     CO.sub.2 Ph  H         O  H     OMe OMe   CH                        I-768                                                                             H     CO.sub.2 Pr  H         O  H     OMe Me    CH                        I-769                                                                             H     CO.sub.2 Pr  H         O  H     OMe OMe   CH                        I-770                                                                             H     CO.sub.2 Pr-i                                                                              H         O  H     OMe Me    CH                        I-771                                                                             H     CO.sub.2 Pr-i                                                                              H         O  H     OMe Me    N                         I-772                                                                             H     CO.sub.2 Pr-i                                                                              H         O  H     OMe OMe   CH                        I-773                                                                             H     COBn         H         O  H     OMe OMe   CH                        I-774                                                                             H     COCH.sub.2 CCH                                                                             H         O  H     OMe OMe   CH                        I-775                                                                             H     COCH.sub.2 CHCH.sub.2                                                                      H         O  H     OMe OMe   CH                        I-776                                                                             H     COEt         H         O  H     OMe OMe   CH                        I-777                                                                             H     COH          H         O  H     OMe OMe   CH                        I-778                                                                             H     COMe         H         O  H     OMe OMe   CH                        I-779                                                                             H     CON(Et).sub.2                                                                              H         O  H     OMe OMe   CH                        I-780                                                                             H     CON(Me).sub.2                                                                              H         O  H     OMe OMe   CH                        I-781                                                                             H     CONH.sub.2   H         O  H     OMe OMe   CH                        I-782                                                                             H     CONHBn       H         O  H     OMe OMe   CH                        I-783                                                                             H     CONHCH.sub.2 C CH                                                                          H         O  H     OMe OMe   CH                        I-784                                                                             H     CONHCH.sub.2 CHCH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-785                                                                             H     CONHEt       H         O  H     OMe OMe   CH                        I-786                                                                             H     CONHMe       H         O  H     OMe OMe   CH                        I-787                                                                             H     CONHOMe      H         O  H     OMe OMe   CH                        I-788                                                                             H     CONHPh       H         O  H     OMe OMe   CH                        I-789                                                                             H     CONHPr       H         O  H     OMe OMe   CH                        I-790                                                                             H     COOMe        H         O  H     OMe Me    CH                        I-791                                                                             H     COOMe        H         O  H     Me  OMe   N                         I-792                                                                             H     COPh         H         O  H     OMe OMe   CH                        I-793                                                                             H     COPr         H         O  H     Me  OMe   CH                        I-794                                                                             H     COPr         H         O  H     Me  OMe   N                         I-795                                                                             H     COPr         H         O  H     OMe OMe   CH                        I-796                                                                             H     COPr-i       H         O  H     Me  OMe   CH                        I-797                                                                             H     COPr-i       H         O  H     Me  OMe   N                         I-798                                                                             H     COPr-i       H         O  H     OMe OMe   CH                        I-799                                                                             H     Cl           5-Cl      O  H     OMe OMe   CH                        I-800                                                                             H     Cl           H         S  H     Cl  OMe   CH                        I-801                                                                             H     Cl           H         O  H     Me  Me    CH                        I-802                                                                             H     Cl           H         O  H     OMe Me    CH                        I-803                                                                             H     Cl           H         O  H     OMe Me    N                         I-804                                                                             H     Cl           H         S  H     Me  Me    CH                        I-805                                                                             H     Cl           H         S  H     OMe Me    CH                        I-806                                                                             H     Cl           H         S  H     OMe Me    N                         I-807                                                                             H     Cl           H         O  Me    OMe OMe   CH                        I-808                                                                             H     Cl           H         S  H     OMe OMe   CH                        I-809                                                                             H     Et           H         O  H     Me  OMe   CH                        I-810                                                                             H     Et           H         O  H     Me  OMe   N                         I-811                                                                             H     Et           H         O  H     OMe OMe   CH                        I-812                                                                             H     F            H         O  H     Me  Me    CH                        I-813                                                                             H     F            H         O  H     OMe Me    CH                        I-814                                                                             H     F            H         O  H     OMe Me    N                         I-815                                                                             H     F            H         O  H     OMe OMe   CH                        I-816                                                                             H     H            5-Cl      O  H     Me  Me    CH                        I-817                                                                             H     H            5-Cl      O  H     OMe Me    N                         I-818                                                                             H     H            5-Cl      O  H     OMe OMe   CH                        I-819                                                                             H     H            5-F       O  H     Me  Me    CN                        I-820                                                                             H     H            5-F       O  H     OMe Me    CH                        I-821                                                                             H     H            5-F       O  H     OMe Me    N                         I-822                                                                             H     H            5-F       O  H     OMe OMe   CH                        I-823                                                                             H     H            5-OEt     O  H     OMe Me    CH                        I-824                                                                             H     H            5-OEt     O  H     OMe Me    N                         I-825                                                                             H     H            5-OEt     O  H     OMe OMe   CH                        I-826                                                                             H     H            5-OEt     O  H     OMe OMe   N                         I-827                                                                             H     H            5-OMe     O  H     Cl  OMe   CH                        I-828                                                                             H     H            5-OMe     O  H     OMe Me    CH                        I-829                                                                             H     H            5-OMe     O  H     OMe Me    N                         I-830                                                                             H     H            5-OMe     O  H     OMe OMe   CH                        I-831                                                                             H     H            5-OPr     O  H     OMe Me    CH                        I-832                                                                             H     H            5-OPr     O  H     OMe Me    N                         I-833                                                                             H     H            5-OPr     O  H     OMe OMe   CH                        I-834                                                                             H     H            5-OPr     O  H     OMe OMe   N                         I-835                                                                             H     H            6-Cl      O  H     Me  Me    CH                        I-836                                                                             H     H            6-Cl      O  H     OMe Me    N                         I-837                                                                             H     H            6-Cl      O  H     OMe OMe   CH                        I-838                                                                             H     H            7-Cl      O  H     OMe Me    N                         I-839                                                                             H     H            7-Cl      O  H     OMe OMe   CH                        I-840                                                                             H     H            H         O  H     OMe Me    CH                        I-841                                                                             H     H            H         O  H     OMe Me    N                         I-842                                                                             H     H            H         O  H     OMe OMe   CH                        I-843                                                                             H     I            H         O  H     Me  OMe   CH                        I-844                                                                             H     I            H         O  H     Me  OMe   N                         I-845                                                                             H     I            H         O  H     OMe OMe   CH                        I-846                                                                             H     Me           H         O  H     OMe OMe   CH                        I-847                                                                             H     N(Et)SO.sub.2 Et                                                                           H         O  H     Me  OMe   CH                        I-848                                                                             H     N(Et)SO.sub.2 Et                                                                           H         O  H     Me  OMe   N                         I-849                                                                             H     N(Et)SO.sub.2 Et                                                                           H         O  H     OMe OMe   CH                        I-850                                                                             H     N(Et)SO.sub.2 Me                                                                           H         O  H     Me  OMe   CH                        I-851                                                                             H     N(Et)SO.sub.2 Me                                                                           H         O  H     Me  OMe   N                         I-852                                                                             H     N(Et)SO.sub.2 Me                                                                           H         O  H     OMe OMe   CH                        I-853                                                                             H     N(Me).sub.2  H         O  H     OMe OMe   CH                        I-854                                                                             H     N(Me)SO.sub.2 Et                                                                           H         O  H     Me  OMe   CH                        I-855                                                                             H     N(Me)SO.sub.2 Et                                                                           H         O  H     Me  OMe   N                         I-856                                                                             H     N(Me)SO.sub.2 Et                                                                           H         O  H     OMe OMe   CH                        I-857                                                                             H     N(Me)SO.sub.2 Me                                                                           H         O  H     Me  OMe   CH                        I-858                                                                             H     N(Me)SO.sub.2 Me                                                                           H         O  H     Me  OMe   N                         I-859                                                                             H     N(Me)SO.sub.2 Me                                                                           H         O  H     OMe OMe   CH                        I-860                                                                             H     NCHPh        H         O  H     Me  OMe   CH                        I-861                                                                             H     NCHPh        H         O  H     Me  OMe   N                         I-862                                                                             H     NCHPh        H         O  H     OMe OMe   CH                        I-863                                                                             H     NCHMe        H         O  H     Me  OMe   CH                        I-864                                                                             H     NCHMe        H         O  H     OMe OMe   N                         I-865                                                                             H     NCHMe        H         O  H     OMe OMe   CH                        I-866                                                                             H     N.sub.3      H         O  H     Me  OMe   CH                        I-867                                                                             H     N.sub.3      H         O  H     Me  OMe   N                         I-868                                                                             H     N.sub.3      H         O  H     OMe OMe   CH                        I-869                                                                             H     NEt.sub.2    H         O  H     OMe OMe   CH                        I-870                                                                             H     NH.sub.2     H         O  H     OMe OMe   CH                        I-871                                                                             H     NHBn         H         O  H     Cl  OMe   CH                        I-872                                                                             H     NHBn         H         O  H     OMe OMe   CH                        I-873                                                                             H     NHCOCF.sub.3 H         O  H     Me  OMe   CH                        I-874                                                                             H     NHCOCF.sub.3 H         O  H     Me  OMe   N                         I-875                                                                             H     NHCOCF.sub.3 H         O  H     OMe OMe   CH                        I-876                                                                             H     NHCOCH.sub.2 Cl                                                                            H         O  H     OMe OMe   CH                        I-877                                                                             H     NHCOEt       H         O  H     Me  OMe   CH                        I-878                                                                             H     NHCOEt       H         O  H     Me  OMe   N                         I-879                                                                             H     NHCOEt       H         O  H     OMe OMe   CH                        I-880                                                                             H     NHCOMe       H         O  H     OMe OMe   CH                        I-881                                                                             H     NHCOOEt      H         O  H     Me  OMe   CH                        I-882                                                                             H     NHCOOEt      H         O  H     Me  OMe   N                         I-883                                                                             H     NHCOOEt      H         O  H     OMe OMe   CH                        I-884                                                                             H     NHCOOMe      H         O  H     Me  OMe   CH                        I-885                                                                             H     NHCOOMe      H         O  H     Me  OMe   N                         I-886                                                                             H     NHCOOMe      H         O  H     OMe OMe   CH                        I-887                                                                             H     NHCOOPh      H         O  H     Me  OMe   CH                        I-888                                                                             H     NHCOOPh      H         O  H     Me  OMe   N                         I-889                                                                             H     NHCOOPh      H         O  H     OMe OMe   CH                        I-890                                                                             H     NHCOPh       H         O  H     OMe OMe   CH                        I-891                                                                             H     NHEt         H         O  H     Me  OMe   CH                        I-892                                                                             H     NHEt         H         O  H     Me  OMe   N                         I-893                                                                             H     NHEt         H         O  H     OMe OMe   CH                        I-894                                                                             H     NHMe         H         O  H     OMe Me    CH                        I-895                                                                             H     NHMe         H         O  H     OMe Me    N                         I-896                                                                             H     NHMe         H         O  H     OMe OMe   CH                        I-897                                                                             H     NHPr         H         O  H     Me  OMe   CH                        I-898                                                                             H     NHPr         H         O  H     Me  OMe   N                         I-899                                                                             H     NHPr         H         O  H     OMe OMe   CH                        I-900                                                                             H     NHSO.sub.2 CH.sub.3                                                                        H         O  H     OMe OMe   CH                        I-901                                                                             H     NHSO.sub.2 Ph                                                                              H         O  H     OMe OMe   CH                        I-902                                                                             H     NMe.sub.2    H         O  H     Cl  OMe   CH                        I-903                                                                             H     NMe.sub.2    H         O  H     Me  Me    CH                        I-904                                                                             H     NMe.sub.2    H         O  H     OMe Me    N                         I-905                                                                             H     NO.sub.2     H         O  H     OMe Me    CH  208-210               I-906                                                                             H     NO.sub.2     H         O  H     OMe OMe   CH  184-186               I-907                                                                             H     OBn          H         O  H     OMe OMe   CH                        I-908                                                                             H     OBn(2-Me)    H         O  H     OMe OMe   CH                        I-909                                                                             H     OBn(3-OMe)   H         O  H     OMe OMe   CH                        I-910                                                                             H     OBn(4-Cl)    H         O  H     OMe OMe   CH                        I-911                                                                             H     OBu          H         O  H     Cl  OMe   CH                        I-912                                                                             H     OBu          H         O  H     Me  Me    CH                        I-913                                                                             H     OBu          H         O  H     OMe Me    CH                        I-914                                                                             H     OBu          H         O  H     OMe Me    N                         I-915                                                                             H     OBu          H         O  H     OMe OMe   CH                        I-916                                                                             H     OCF.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   CH                        I-917                                                                             H     OCF.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   N                         I-918                                                                             H     OCF.sub.2 CH.sub.2 Cl                                                                      H         O  H     OMe OMe   CH                        I-919                                                                             H     OCF.sub.2 CHFCl                                                                            H         O  H     Me  OMe   CH                        I-920                                                                             H     OCF.sub.2 CHFCl                                                                            H         O  H     Me  OMe   N                         I-921                                                                             H     OCF.sub.2 CHFCl                                                                            H         O  H     OMe OMe   CH                        I-922                                                                             H     OCF.sub.3    H         O  H     Me  OMe   CH                        I-923                                                                             H     OCF.sub.3    H         O  H     Me  OMe   N                         I-924                                                                             H     OCF.sub.3    H         O  H     OMe OMe   CH                        I-925                                                                             H     OCH(CF.sub.2 CF.sub.3)Me                                                                   H         O  H     Me  OMe   CH                        I-926                                                                             H     OCH(CF.sub.2 CF.sub.3)Me                                                                   H         O  H     Me  OMe   N                         I-927                                                                             H     OCH(CF.sub.2 CF.sub.3 )Me                                                                  H         O  H     OMe OMe   CH                        I-928                                                                             H     OCH(CF.sub.3)Me                                                                            H         O  H     OMe Me    CH                        I-929                                                                             H     OCH(CF.sub.3)Me                                                                            H         O  H     OMe OMe   CH                        I-930                                                                             H     OCH.sub.2 C(Cl)CH.sub.2                                                                    H         O  H     Me  OMe   CH                        I-931                                                                             H     OCH.sub.2 C(Cl)CH.sub.2                                                                    H         O  H     Me  OMe   N                         I-932                                                                             H     OCH.sub.2 C(Cl)CH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-933                                                                             H     OCH.sub.2 C(Me)CH.sub.2                                                                    H         O  H     Me  OMe   CH                        I-934                                                                             H     OCH.sub.2 C(Me)CH.sub.2                                                                    H         O  H     Me  OMe   N                         I-935                                                                             H     OCH.sub.2 C(Me)CH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-936                                                                             H     OCH.sub.2 CCH                                                                              H         O  H     OMe OMe   CH                        I-937                                                                             H     OCH.sub.2 CF.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   CH                        I-938                                                                             H     OCH.sub.2 CF.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   N                         I-939                                                                             H     OCH.sub.2 CF.sub.2 CF.sub.3                                                                H         O  H     OMe OMe   CH                        I-940                                                                             H     OCH.sub.2 CF.sub.2 CHF.sub.2                                                               H         O  H     Me  OMe   CH                        I-941                                                                             H     OCH.sub.2 CF.sub.2 CHF.sub.2                                                               H         O  H     Me  OMe   N                         I-942                                                                             H     OCH.sub.2 CF.sub.2 CHF.sub.2                                                               H         O  H     OMe OMe   CH                        I-943                                                                             H     OCH.sub.2 CF.sub.3                                                                         H         O  H     Cl  OMe   CH                        I-944                                                                             H     OCH.sub.2 CF.sub.3                                                                         H         O  H     OMe Me    CH                        I-945                                                                             H     OCH.sub.2 CF.sub.3                                                                         H         O  H     OMe Me    N                         I-946                                                                             H     OCH.sub.2 CF.sub.3                                                                         H         O  H     OMe OMe   CH                        I-947                                                                             H     OCH.sub.2 CHCCl.sub.2                                                                      H         O  H     Me  OMe   CH                        I-948                                                                             H     OCH.sub.2 CHCCl.sub.2                                                                      H         O  H     Me  OMe   N                         I-949                                                                             H     OCH.sub.2 CHCCl.sub.2                                                                      H         O  H     OMe OMe   CH                        I-950                                                                             H     OCH.sub.2 CHCHCl                                                                           H         O  H     Me  OMe   CH                        I-951                                                                             H     OCH.sub.2 CHCHCl                                                                           H         O  H     Me  OMe   N                         I-952                                                                             H     OCH.sub.2 CHCHCl                                                                           H         O  H     OMe OMe   CH                        I-953                                                                             H     OCH.sub.2 CHCH.sub.2                                                                       H         O  H     OMe OMe   CH                        I-954                                                                             H     OCH.sub.2 CHCHMe                                                                           H         O  H     Me  OMe   CH                        I-955                                                                             H     OCH.sub.2 CHCHMe                                                                           H         O  H     Me  OMe   N                         I-956                                                                             H     OCH.sub.2 CHCHMe                                                                           H         O  H     OMe OMe   CH                        I-957                                                                             H     OCH.sub.2 CH.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   CH                        I-958                                                                             H     OCH.sub.2 CH.sub.2 CF.sub.3                                                                H         O  H     Me  OMe   N                         I-959                                                                             H     OCH.sub.2 CH.sub.2 CF.sub.3                                                                H         O  H     OMe OMe   CH                        I-960                                                                             H     OCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     OMe OMe   CH                        I-961                                                                             H     OCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe OMe   CH                        I-962                                                                             H     OCH.sub.2 CH.sub.2 N.sub.3                                                                 H         O  H     Me  OMe   CH                        I-963                                                                             H     OCH.sub.2 CH.sub.2 N.sub.3                                                                 H         O  H     Me  OMe   N                         I-964                                                                             H     OCH.sub.2 CH.sub.2 N.sub.3                                                                 H         O  H     OMe OMe   CH                        I-965                                                                             H     OCH.sub.2 CH.sub.2 NMe.sub.2                                                               H         O  H     OMe Me    CH                        I-966                                                                             H     OCH.sub.2 CH.sub.2 NMe.sub.2                                                               H         O  H     OMe Me    N                         I-967                                                                             H     OCH.sub.2 CH.sub.2 NMe.sub.2                                                               H         O  H     OMe OMe   CH                        I-968                                                                             H     OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe Me    CH                        I-969                                                                             H     OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe Me    N                         I-970                                                                             H     OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe OMe   CH                        I-971                                                                             H     OCH.sub.2 CH.sub.2 OBu                                                                     H         O  H     OMe OMe   N                         I-972                                                                             H     OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe Me    CH                        I-973                                                                             H     OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe Me    N                         I-974                                                                             H     OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe OMe   CH                        I-975                                                                             H     OCH.sub.2 CH.sub.2 OBu-t                                                                   H         O  H     OMe OMe   N                         I-976                                                                             H     OCH.sub.2 CH.sub.2 OEt                                                                     H         O  H     OMe Me    CH                        I-977                                                                             H     OCH.sub.2 CH.sub.2 OEt                                                                     H         O  H     OMe Me    N                         I-978                                                                             H     OCH.sub.2 CH.sub.2 OEt                                                                     H         O  H     OMe OMe   CH                        I-979                                                                             H     OCH.sub.2 CH.sub.2 OMe                                                                     H         O  H     OMe Me    CH                        I-980                                                                             H     OCH.sub.2 CH.sub.2 OMe                                                                     H         O  H     OMe OMe   CH                        I-981                                                                             H     OCH.sub.2 CH.sub.2 OPh                                                                     H         O  H     OMe OMe   CH                        I-982                                                                             H     OCH.sub.2 CH.sub.2 OPr-i                                                                   H         O  H     OMe Me    CH                        I-983                                                                             H     OCH.sub.2 CH.sub.2 OPr-i                                                                   H         O  H     OMe Me    N                         I-984                                                                             H     OCH.sub.2 CH.sub.2 OPr-i                                                                   H         O  H     OMe OMe   CH                        I-985                                                                             H     OCH.sub.2 CH.sub.2 SMe                                                                     H         O  H     Me  OMe   CH                        I-986                                                                             H     OCH.sub.2 CH.sub.2 SMe                                                                     H         O  H     Me  OMe   N                         I-987                                                                             H     OCH.sub.2 CH.sub.2 SMe                                                                     H         O  H     OMe OMe   CH                        I-988                                                                             H     OCH.sub.2 CHCl.sub.2                                                                       H         O  H     Me  OMe   CH                        I-989                                                                             H     OCH.sub.2 CHCl.sub.2                                                                       H         O  H     Me  OMe   N                         I-990                                                                             H     OCH.sub.2 CHCl.sub.2                                                                       H         O  H     OMe OMe   CH                        I-991                                                                             H     OCH.sub.2 CHF.sub.2                                                                        H         O  H     Me  OMe   CH                        I-992                                                                             H     OCH.sub.2 CHF.sub.2                                                                        H         O  H     Me  OMe   N                         I-993                                                                             H     OCH.sub.2 CHF.sub.2                                                                        H         O  H     OMe OMe   CH                        I-994                                                                             H     OCH.sub.2 CN H         O  H     Me  OMe   CH                        I-995                                                                             H     OCH.sub.2 CN H         O  H     Me  OMe   N                         I-996                                                                             H     OCH.sub.2 CN H         O  H     OMe OMe   CH                        I-997                                                                             H     OCH.sub.2 COOEt                                                                            H         O  H     OMe OMe   CH                        I-998                                                                             H     OCH.sub.2 COOMe                                                                            H         O  H     Me  OMe   CH                        I-999                                                                             H     OCH.sub.2 COOMe                                                                            H         O  H     Me  OMe   N                         I-1000                                                                            H     OCH.sub.2 COOMe                                                                            H         O  H     OMe OMe   CH                        I-1001                                                                            H     OCH.sub.2 COOPr                                                                            H         O  H     Me  OMe   CH                        I-1002                                                                            H     OCH.sub.2 COOPr                                                                            H         O  H     Me  OMe   N                         I-1003                                                                            H     OCH.sub.2 COOPr                                                                            H         O  H     OMe OMe   CH                        I-1004                                                                            H     OCH.sub.2 COOPr-i                                                                          H         O  H     Me  OMe   CH                        I-1005                                                                            H     OCH.sub.2 COOPr-i                                                                          H         O  H     Me  OMe   N                         I-1006                                                                            H     OCH.sub.2 COOPr-i                                                                          H         O  H     OMe OMe   CH                        I-1007                                                                            H     OCH.sub.2 OBn                                                                              H         O  H     Me  OMe   CH                        I-1008                                                                            H     OCH.sub.2 OBn                                                                              H         O  H     Me  OMe   N                         I-1009                                                                            H     OCH.sub.2 OBn                                                                              H         O  H     OMe OMe   CH                        I-1010                                                                            H     OCH.sub.2 OBu-t                                                                            H         O  H     Me  OMe   CH                        I-1011                                                                            H     OCH.sub.2 OBu-t                                                                            H         O  H     Me  OMe   N                         I-1012                                                                            H     OCH.sub.2 OBu-t                                                                            H         O  H     OMe OMe   CH                        I-1013                                                                            H     OCH.sub.2 OCH.sub.2 CF.sub.3                                                               H         O  H     Me  OMe   CH                        I-1014                                                                            H     OCH.sub.2 OCH.sub.2 CF.sub.3                                                               H         O  H     Me  OMe   N                         I-1015                                                                            H     OCH.sub.2 OCH.sub.2 CF.sub.3                                                               H         O  H     OMe OMe   CH                        I-1016                                                                            H     OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                           H         O  H     Me  OMe   CH                        I-1017                                                                            H     OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                           H         O  H     Me  OMe   N                         I-1018                                                                            H     OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                           H         O  H     OMe OMe   CH                        I-1019                                                                            H     OCH.sub.2 OEt                                                                              H         O  H     Me  OMe   CH                        I-1020                                                                            H     OCH.sub.2 OEt                                                                              H         O  H     Me  OMe   N                         I-1021                                                                            H     OCH.sub.2 OEt                                                                              H         O  H     OMe OMe   CH                        I-1022                                                                            H     OCH.sub.2 OMe                                                                              H         O  H     Me  OMe   CH                        I-1023                                                                            H     OCH.sub.2 OMe                                                                              H         O  H     Me  OMe   N                         I-1024                                                                            H     OCH.sub.2 OMe                                                                              H         O  H     OMe OMe   CH                        I-1025                                                                            H     OCH.sub.2 SMe                                                                              H         O  H     Me  OMe   CH                        I-1026                                                                            H     OCH.sub.2 SMe                                                                              H         O  H     Me  OMe   N                         I-1027                                                                            H     OCH.sub.2 SMe                                                                              H         O  H     OMe OMe   CH                        I-1028                                                                            H     OCHF.sub.2   H         O  H     Me  OMe   CH                        I-1029                                                                            H     OCHF.sub.2   H         O  H     Me  OMe   N                         I-1030                                                                            H     OCHF.sub.2   H         O  H     OMe OMe   CH                        I-1031                                                                            H     OCOEt        H         O  H     Me  OMe   CH                        I-1032                                                                            H     OCOEt        H         O  H     Me  OMe   N                         I-1033                                                                            H     OCOEt        H         O  H     OMe OMe   CH                        I-1034                                                                            H     OCOMe        H         O  H     OMe OMe   CH                        I-1035                                                                            H     OCONMe.sub.2 H         O  H     Me  OMe   CH                        I-1036                                                                            H     OCONMe.sub.2 H         O  H     Me  OMe   N                         I-1037                                                                            H     OCONMe.sub.2 H         O  H     OMe OMe   CH                        I-1038                                                                            H     OCOPh        H         O  H     Me  OMe   CH                        I-1039                                                                            H     OCOPh        H         O  H     Me  OMe   N                         I-1040                                                                            H     OCOPh        H         O  H     OMe OMe   CH                        I-1041                                                                            H     OCOPr        H         O  H     Me  OMe   CH                        I-1042                                                                            H     OCOPr        H         O  H     Me  OMe   N                         I-1043                                                                            H     OCOPr        H         O  H     OMe OMe   CH                        I-1044                                                                            H     OEt          H         O  H     Me  Me    CH                        I-1045                                                                            H     OEt          H         O  H     OMe Me    CH                        I-1046                                                                            H     OEt          H         O  H     OMe Me    N                         I-1047                                                                            H     OEt          H         O  H     OMe OMe   CH                        I-1048                                                                            H     OH           H         O  H     OMe OMe   CH                        I-1049                                                                            H     OMe          5-Cl      O  H     OMe Me    N                         I-1050                                                                            H     OMe          5-Cl      O  H     OMe OMe   CH                        I-1051                                                                            H     OMe          5-OMe     O  H     OMe Me    CH                        I-1052                                                                            H     OMe          H         O  H     Cl  OMe   CH                        I-1053                                                                            H     OMe          H         O  N     OMe Me    CH                        I-1054                                                                            H     OMe          H         O  H     OMe OMe   N                         I-1055                                                                            H     OMe          H         O  H     Me  Me    CH                        I-1056                                                                            H     OMe          H         O  H     OMe Me    N                         I-1057                                                                            H     OMe          H         O  H     OMe OMe   CH                        I-1058                                                                            H     OPh          H         O  H     OMe OMe   CH                        I-1059                                                                            H     OPh(2-Me)    H         O  H     OMe OMe   CH                        I-1060                                                                            H     OPh(3-OMe)   H         O  H     OMe OMe   CH                        I-1061                                                                            H     OPh(4-Cl)    H         O  H     OMe OMe   CH                        I-1062                                                                            H     OPr          H         O  H     Cl  OMe   CH                        I-1063                                                                            H     OPr          H         O  H     Me  Me    CH                        I-1064                                                                            H     OPr          H         O  H     OMe Me    CH                        I-1065                                                                            H     OPr          H         O  H     OMe Me    N                         I-1066                                                                            H     OPr          H         O  H     OMe OMe   CH                        I-1067                                                                            H     OPr-i        H         O  H     Me  Me    CH                        I-1068                                                                            H     OPr-i        H         O  H     OMe Me    CH                        I-1069                                                                            H     OPr-i        H         O  H     OMe Me    N                         I-1070                                                                            H     OPr-i        H         O  H     OMe OMe   CH                        I-1071                                                                            H     Ph           H         O  H     OMe OMe   CH                        I-1072                                                                            H     Pr           H         O  H     Me  OMe   CH                        I-1073                                                                            H     Pr           H         O  H     Me  OMe   N                         I-1074                                                                            H     Pr           H         O  H     OMe OMe   CH                        I-1075                                                                            H     Pr-i         H         O  H     Me  OMe   CH                        I-1076                                                                            H     Pr-i         H         O  H     Me  OMe   N                         I-1077                                                                            H     Pr-i         H         O  H     OMe OMe   CH                        I-1078                                                                            H     SBu          H         O  H     Cl  OMe   CH                        I-1079                                                                            H     SBu          H         O  H     OMe OMe   CH                        I-1080                                                                            H     SCF.sub.3    H         O  H     Me  OMe   CH                        I-1081                                                                            H     SCF.sub.3    H         O  H     Me  OMe   N                         I-1082                                                                            H     SCF.sub.3    H         O  H     OMe OMe   CH                        I-1083                                                                            H     SCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   CH                        I-1084                                                                            H     SCH.sub.2 CH.sub.2 Cl                                                                      H         O  H     Me  OMe   N                         I-1085                                                                            H     SCH.sub. 2 CH.sub.2 Cl                                                                     H         O  H     OMe OMe   CH                        I-1086                                                                            H     SCH.sub.2 CH.sub.2 F                                                                       H         O  H     Me  OMe   CH                        I-1087                                                                            H     SCH.sub.2 CH.sub.2 F                                                                       H         O  H     Me  OMe   N                         I-1088                                                                            H     SCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe OMe   CH                        I-1089                                                                            H     SEt          H         O  H     OMe Me    N                         I-1090                                                                            H     SEt          H         O  H     OMe OMe   CH                        I-1091                                                                            H     SH           H         O  H     OMe OMe   CH                        I-1092                                                                            H     SMe          H         O  H     OMe OMe   CH                        I-1093                                                                            H     SO.sub.2 Bu  H         O  H     OMe OMe   CH                        I-1094                                                                            H     SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     Me  OMe   CH                        I-1095                                                                            H     SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     Me  OMe   N                         I-1096                                                                            H     SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H         O  H     OMe OMe   CH                        I-1097                                                                            H     SO.sub.2 Et  H         O  H     OMe OMe   CH                        I-1098                                                                            H     SO.sub.2 Me  H         O  H     OMe OMe   CH                        I-1099                                                                            H     SO.sub.2 NMe.sub.2                                                                         H         O  H     OMe OMe   CH                        I-1100                                                                            H     SO.sub.2 NEt.sub.2                                                                         H         O  H     Me  OMe   CH                        I-1101                                                                            H     SO.sub.2 NEt.sub.2                                                                         H         O  H     Me  OMe   N                         I-1102                                                                            H     SO.sub.2 NEt.sub.2                                                                         H         O  H     OMe OMe   CH                        I-1103                                                                            H     SO.sub.2 NH.sub.2                                                                          H         O  H     OMe OMe   CH                        I-1104                                                                            H     SO.sub.2 NHBn                                                                              H         O  H     OMe OMe   CH                        I-1105                                                                            H     SO.sub.2 NHCH.sub.2 CCH                                                                    H         O  H     OMe OMe   CH                        I-1106                                                                            H     SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                             H         O  H     OMe OMe   CH                        I-1107                                                                            H     SO.sub.2 NHMe                                                                              H         O  H     OMe OMe   CH                        I-1108                                                                            H     SO.sub.2 NHOEt                                                                             H         O  H     Me  OMe   CH                        I-1109                                                                            H     SO.sub.2 NHOEt                                                                             H         O  H     Me  OMe   N                         I-1110                                                                            H     SO.sub.2 NHOEt                                                                             H         O  H     OMe OMe   CH                        I-1111                                                                            H     SO.sub.2 NHOMe                                                                             H         O  H     OMe OMe   CH                        I-1112                                                                            H     SO.sub.2 NHPh                                                                              H         O  H     OMe OMe   CH                        I-1113                                                                            H     SO.sub.2 Pr  H         O  H     OMe OMe   CH                        I-1114                                                                            H     SO.sub.2 Pr-i                                                                              H         O  H     Cl  OMe   CH                        I-1115                                                                            H     SO.sub.2 Pr-i                                                                              H         O  H     OMe OMe   CH                        I-1116                                                                            H     SOEt         H         O  H     Me  OMe   CH                        I-1117                                                                            H     SOEt         H         O  H     Me  OMe   N                         I-1118                                                                            H     SOEt         H         O  H     OMe OMe   CH                        I-1119                                                                            H     SOMe         H         O  H     OMe OMe   CH                        I-1120                                                                            H     SPr          H         O  H     Cl  OMe   CH                        I-1121                                                                            H     SPr          H         O  H     OMe Me    CH                        I-1122                                                                            H     SPr          H         O  H     OMe Me    N                         I-1123                                                                            H     SPr          H         O  H     OMe OMe   CH                        I-1124                                                                            H     SPr-i        H         O  H     Cl  OMe   CH                        I-1125                                                                            H     SPr-i        H         O  H     OMe OMe   CH                        I-1126                                                                            H     NO.sub.2     H         O  H     Me  OMe   N   182-184               I-1127                                                                            H     SEt          H         O  H     Cl  OMe   CH                        I-1128                                                                            H     SEt          H         O  H     Me  Me    CH                        I-1129                                                                            H     SEt          H         O  H     OMe OMe   N                         I-1130                                                                            H     SBu          H         O  H     OMe Me    CH                        I-1131                                                                            H     SBu          H         O  H     OMe Me    N                         I-1132                                                                            H     SPr-i        H         O  H     OMe Me    CH                        I-1133                                                                            H     SPr-i        H         O  H     OMe Me    N                         I-1134                                                                            H     SOEt         H         O  H     OMe OMe   N                         I-1135                                                                            H     SO.sub.2 Et  H         O  H     OMe Me    CH                        I-1136                                                                            H     SO.sub.2 Et  H         O  H     OMe Me    N                         I-1137                                                                            H     SO.sub.2 Et  H         O  H     OMe Cl    CH                        I-1138                                                                            H     SO.sub.2 Pr  H         O  H     OMe Me    CH                        I-1139                                                                            H     SO.sub.2 Pr  H         O  H     OMe Me    N                         I-1140                                                                            H     SO.sub.2 Pr  H         O  H     OMe Cl    CH                        I-1141                                                                            H     SO.sub.2 Bu  H         O  H     OMe Me    CH                        I-1142                                                                            H     SO.sub.2 Bu  H         O  H     OMe Me    N                         I-1143                                                                            H     SO.sub.2 Bu  H         O  H     OMe Cl    CH                        I-1144                                                                            H     SO.sub.2 Pr-i                                                                              H         O  H     OMe Me    CH                        I-1145                                                                            H     SO.sub.2 Pr-i                                                                              H         O  H     OMe Me    N                         I-1146                                                                            H     COOPr        H         O  H     OMe Me    N                         I-1147                                                                            H     NO.sub.2     H         O  H     OMe Cl    CH                        I-1148                                                                            H     CONMe.sub.2  H         O  H     OMe Me    CH                        I-1149                                                                            H     Br           H         O  H     OMe Cl    CH                        I-1150                                                                            H                                                                                    ##STR29##   H         O  H     OMe OMe   CH                        I-1151                                                                            H     OCH.sub.2Bu-t                                                                              H         O  H     OMe OMe   CH                        I-1152                                                                            H     OCH.sub.2Bu-t                                                                              H         O  H     Me  OMe   CH                        I-1153                                                                            H     OCH.sub.2 CHCMe.sub.2                                                                      H         O  H     OMe OMe   CH                        I-1154                                                                            H     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                              H         O  H     OMe OMe   CH                        I-1155                                                                            H     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                              H         O  H     Me  OMe   CH                        I-1156                                                                            H     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                              H         O  H     Me  OMe   N                         I-1157                                                                            H     CH.sub.2 CH.sub.2 N.sub.3                                                                  H         O  H     OMe OMe   CH                        I-1158                                                                            H                                                                                    ##STR30##   H         O  H     OMe OMe   CH                        I-1159                                                                            H     COCF.sub.3   H         O  H     OMe OMe   CH                        I-1160                                                                            H     COOCH.sub.2 CHCHCl                                                                         H         O  H     OMe OMe   CH                        I-1161                                                                            H     SO.sub.2 CF.sub.3                                                                          H         O  H     OMe OMe   CH                        I-1162                                                                            H     OCOCF.sub.3  H         O  H     OMe OMe   CH                        I-1163                                                                            H     OCH.sub.2 OPh                                                                              H         O  H     OMe OMe   CH                        I-1164                                                                            H     CHNOH        H         O  H     OMe OMe   CH                        I-1165                                                                            H     CHNOCH.sub.2 CHCH.sub.2                                                                    H         O  H     OMe OMe   CH                        I-1166                                                                            H     CHNOCH.sub.2 CCH                                                                           H         O  H     OMe OMe   CH                        I-1167                                                                            H     C(Me)NOBn    H         O  H     OMe OMe   CH                        I-1168                                                                            H     C(Me)NOPh    H         O  H     OMe OMe   CH                        I-1169                                                                            H     C(Bn)NOMe    H         O  H     OMe OMe   CH                        I-1170                                                                            H     C(Ph)NOMe    H         O  H     OMe OMe   CH                        I-1171                                                                            H     C(CF.sub.3)NOMe                                                                            H         O  H     OMe OMe   CH                        I-1172                                                                            H     COOCH.sub.2 CH.sub.2 Cl                                                                    H         O  H     OMe OMe   CH                        I-1173                                                                            H     COOCH.sub.2 CF.sub.3                                                                       H         O  H     OMe OMe   CH                        I-1174                                                                            H     Cl           S-Cl      O  H     OMe Me    N                         I-1175                                                                            H     Cl           5-OMe     O  H     OMe OMe   CH                        I-1176                                                                            H     Cl           5-F       O  H     OMe OMe   CH                        I-1177                                                                            H     F            5-Cl      O  H     OMe OMe   CH                        I-1178                                                                            H     F            5-F       O  H     OMe OMe   CH                        I-1179                                                                            H     COOMe        5-Cl      O  H     OMe OMe   CH                        I-1180                                                                            H     COOEt        5-Cl      O  H     OMe OMe   CH                        I-1181                                                                            H     COOPr        5-Cl      O  H     OMe OMe   CH                        I-1182                                                                            H     COOPr-i      5-Cl      O  H     OMe OMe   CH                        I-1183                                                                            H     OMe          5-COOMe   O  H     OMe OMe   CH                        I-1184                                                                            H     COOMe        5-OMe     O  H     OMe OMe   CH                        I-1185                                                                            H     ONCHOMe      H         O  H     OMe OMe   CH                        I-1186                                                                            H     ONCMe.sub.2  H         O  H     OMe OMe   CH                        I-1187                                                                            H     ONCHBn       H         O  H     OMe OMe   CH                        I-1188                                                                            H     OCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe Me    CH                        I-1189                                                                            H     OCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe Me    N                         I-1190                                                                            H     H            5-CN      O  H     OMe OMe   CH                        I-1191                                                                            H     H            5-CF.sub.3                                                                              O  H     OMe OMe   CH                        I-1192                                                                            H     H            5-COOMe   O  H     OMe OMe   CH                        I-1193                                                                            H     H            5-COOEt   O  H     OMe OMe   CH                        I-1194                                                                            H     H            5-COOPr   O  H     OMe OMe   CH                        I-1195                                                                            H     H            5-COOPr-i O  H     OMe OMe   CH                        I-1196                                                                            H     H            5-COOCH.sub.2 CH.sub.2 Cl                                                               O  H     OMe OMe   CH                        I-1197                                                                            H     H            5-COOCH.sub.2 CH.sub.2 F                                                                O  H     OMe OMe   CH                        I-1198                                                                            H     H            5-COOCH.sub.2 CF.sub.3                                                                  O  H     OMe OMe   CH                        I-1199                                                                            H     H            5-COOCH.sub.2 OMe                                                                       O  H     OMe OMe   CH                        I-1200                                                                            H     H            5-CONMe.sub.2                                                                           O  H     OMe OMe   CH                        I-1201                                                                            H     H            5-OCH.sub.2 CH.sub.2 F                                                                  O  H     OMe OMe   CH                        I-1202                                                                            H     H            5-OCHF.sub.2                                                                            O  H     OMe OMe   CH                        I-1203                                                                            H     H            5-OCH.sub.2 CF.sub.3                                                                    O  H     OMe OMe   CH                        I-1204                                                                            H     H            5-OCH.sub.2 CH.sub.2 CH.sub.2 F                                                         O  H     OMe OMe   CH                        I-1205                                                                            H     H            5-OCH.sub.2 CHCH.sub.2                                                                  O  H     OMe OMe   CH                        I-1206                                                                            H     H            5-OCH.sub.2 CCH                                                                         O  H     OMe OMe   CH                        I-1207                                                                            H     H            5-NO.sub.2                                                                              O  H     OMe OMe   CH                        I-1208                                                                            H     H            5-SMe     O  H     OMe OMe   CH                        I-1209                                                                            H     H            5-SEt     O  H     OMe OMe   CH                        I-1210                                                                            H     H            5-SPr     O  H     OMe OMe   CH                        I-1211                                                                            H     H            5-SPr-i   O  H     OMe OMe   CH                        I-1212                                                                            H     H            5-SO.sub.2 Et                                                                           O  H     OMe OMe   CH                        I-1213                                                                            H     H            5-SO.sub.2 Pr                                                                           O  H     OMe OMe   CH                        I-1214                                                                            H     H            5-SO.sub.2 Pr-i                                                                         O  H     OMe OMe   CH                        I-1215                                                                            H     H            5-SOEt    O  H     OMe OMe   CH                        I-1216                                                                            H     H            5-Me      O  H     OMe OMe   CH                        I-1217                                                                            H     H            5-Et      O  H     OMe OMe   CH                        I-1218                                                                            H     H            5-Pr      O  H     OMe OMe   CH                        I-1219                                                                            H     H            5-SO.sub.2 NMe.sub.2                                                                    O  H     OMe OMe   CH                        I-1220                                                                            H     H            5-OCF.sub.3                                                                             O  H     OMe OMe   CH                        I-1221                                                                            H     H            5-CH.sub.2 CF.sub.3                                                                     O  H     OMe OMe   CH                        I-1222                                                                            H     H            5-CH.sub.2 CHCH.sub.2                                                                   O  H     OMe OMe   CH                        I-1223                                                                            H     H            5-COOMe   O  H     OMe Me    CH                        I-1224                                                                            H     H            5-COOMe   O  H     OMe Me    N                         I-1225                                                                            H     H            5-COOMe   O  H     OMe OMe   M                         I-1226                                                                            H     Cl           H         O  CH.sub.3 OCH.sub.2                                                                  OMe OMe   CH                        I-1227                                                                            H     Cl           H         O  H     OMe NMe.sub.2                                                                           N                         I-1228                                                                            H     Cl           H         O  H     OMe NHMe  N                         I-1229                                                                            H                                                                                    ##STR31##   H         O  H     Me  OMe   CH                        I-1230                                                                            H                                                                                    ##STR32##   H         O  H     Me  OMe   N                         I-1231                                                                            H                                                                                    ##STR33##   H         O  H     OMe OMe   CH                        I-1232                                                                            H                                                                                    ##STR34##   H         O  H     OMe OMe   CH                        I-1233                                                                            H                                                                                    ##STR35##   H         O  H     Me  OMe   CH                        I-1234                                                                            H                                                                                    ##STR36##   H         O  H     Me  OMe   N                         I-1235                                                                            H                                                                                    ##STR37##   H         O  H     OMe OMe   CH                        I-1236                                                                            H                                                                                    ##STR38##   H         O  H     Me  OMe   CH                        I-1237                                                                            H                                                                                    ##STR39##   H         O  H     Me  OMe   N                         I-1238                                                                            H                                                                                    ##STR40##   H         O  H     OMe OMe   CH                        I-1239                                                                            H                                                                                    ##STR41##   H         O  H     Me  OMe   CH                        I-1240                                                                            H                                                                                    ##STR42##   H         O  H     Me  OMe   N                         I-1241                                                                            H     OC.sub.2 H.sub.4  O*   O  H     OMe OMe   CH                        I-1242                                                                            H     OC.sub.2 H.sub.4 O*    O  H     Me  OMe   CH                        I-1243                                                                            H     OC.sub.2 H.sub.4 O*    O  H     Me  OMe   N                         I-1244                                                                            H     SC.sub.2 H.sub.4 S*    O  H     OMe OMe   CH                        I-1243                                                                            H     SC.sub.2 H.sub.4 S*    O  H     Me  OMe   CH                        I-1246                                                                            H     SC.sub.2 H.sub.4 S*    O  H     Me  OMe   N                         I-1247                                                                            H     OCH.sub.2 O*           O  H     OMe OMe   CH                        I-1248                                                                            Me    Cl           H         O  CH.sub.3 OCH.sub.2                                                                  OMe OMe   CH                        I-1249                                                                            Me    Cl           H         O  H     OMe NMe.sub.2                                                                           N                         I-1250                                                                            Me    Cl           H         O  H     OMe NHMe  N                         I-1251                                                                            Me    ONCHMe       H         O  H     OMe OMe   CH                        I-1252                                                                            Me    ONCOMe.sub.2 H         O  H     OMe OMe   CH                        I-1253                                                                            Me    ONCHBn       H         O  H     OMe OMe   CH                        I-1254                                                                            Me    OCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe Me    CH                        I-1255                                                                            Me    OCH.sub.2 CH.sub.2 F                                                                       H         O  H     OMe Me    N                         I-1256                                                                            Me    F            H         O  H     NMe.sub.2                                                                         OCH.sub.2 CF.sub.3                                                                  N   128-130               I-1257                                                                            Me    CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                              H         O  H     OMe OMe   CH                        I-1258                                                                            Me    CO.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     OMe OMe   CH                        I-1259                                                                            Me    CO.sub.2 CH.sub.2 OMe                                                                      H         O  H     OMe OMe   CH                        I-1260                                                                            H     CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                              H         O  H     OMe OMe   CH                        I-1261                                                                            H     CO.sub.2 CH.sub.2 CF.sub.3                                                                 H         O  H     OMe OMe   CH                        I-1262                                                                            H     CO.sub.2 CH.sub.2 OMe                                                                      H         O  H     OMe OMe   CH                        I-1263                                                                            Et    CO.sub.2 Me  H         O  H     OMe Me    CH  198-200               I-1264                                                                            Et    CO.sub.2 Me  H         O  H     OMe Me    N   153-105               I-1265                                                                            Me    SO.sub.2 NMe.sub.2                                                                         H         O  H     OMe Me    CH  134-135               I-1266                                                                            Me    SO.sub.2 NMe.sub.2                                                                         H         O  H     OMe Me    N   253-255               __________________________________________________________________________     *R.sup.3 represents the 5position.                                       

                                      TABLE 2                                     __________________________________________________________________________     ##STR43##                                                                    Comp.                                                                         No. R.sup.1 R.sup.2     R.sup.3    X Y     A    B      Z  mp.                 __________________________________________________________________________                                                              (°C.)        II-1                                                                              Me      Ph          H          O H     OMe  OMe    CH                     II-2                                                                              Me      Bn          H          O H     OMe  OMe    CH                     II-3                                                                              Me      SH          H          O H     OMe  OMe    CH                     II-4                                                                              Me      SMe         H          O H     OMe  OMe    CH                     II-5                                                                              Me      SEt         H          O H     OMe  OMe    CH 156-157             II-6                                                                              Me      SPr         H          O H     OMe  OMe    CH 143-145             II-7                                                                              Me      SO.sub.2 Me H          O H     OMe  OMe    CH                     II-8                                                                              Me      SO.sub.2 Et H          O H     OMe  OMe    CH 196-198             II-9                                                                              Me      SOMe        H          O H     OMe  OMe    CH                     II-10                                                                             Me      SO.sub.2 NHMe                                                                             H          O H     OMe  OMe    CH                     II-11                                                                             Me      SO.sub.2 NHOMe                                                                            H          O H     OMe  OMe    CH                     II-12                                                                             Me      SO.sub.2 NMe.sub.2                                                                        H          O H     OMe  OMe    CH 169-171             II-13                                                                             Me      SO.sub.2 NHBn                                                                             H          O H     OMe  OMe    CH                     II-14                                                                             Me      SO.sub.2 NHPh                                                                             H          O H     OMe  OMe    CH                     II-15                                                                             Me      SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                            H          O H     OMe  OMe    CH                     II-16                                                                             Me      SO.sub.2 NHCH.sub.2 CH                                                                    H          O H     OMe  OMe    CH                     II-17                                                                             H       Cl          H          O H     OMe  OMe    CH 191-193             II-18                                                                             Me      Cl          H          O H     Me   Me     CH 210-213             II-19                                                                             Me      Cl          5-Cl       O H     OMe  OMe    CH 203-205             II-20                                                                             Et      Cl          H          O H     OMe  OMe    CH 174-175             II-21                                                                             Ph      Cl          H          O H     OMe  OMe    CH 221-223             II-22                                                                             Bn      Cl          H          O H     OMe  OMe    CH                     II-23                                                                             Me      H           H          O H     OMe  OMe    CH 199-202             II-24                                                                             Me      H           H          O H     Me   Me     CH 208-210             II-25                                                                             Me      H           H          O H     OMe  Me     N  172-174             II-26                                                                             Me      F           H          O H     OMe  OMe    CH 205-206             II-27                                                                             Me      Br          H          O H     OMe  OMe    CH 179-182             II-28                                                                             Me      Me          H          O H     OMe  OMe    CH 178-180             II-29                                                                             Me      CN          H          O H     OMe  OMe    CH 189-191             II-30                                                                             Me      CF.sub.3    H          O H     OMe  OMe    CH                     II-31                                                                             Me      Cl          H          O H     OMe  Me     CH 202-204             II-32                                                                             Me      Cl          H          O H     OMe  Me     N  170-172             II-33                                                                             Me      F           H          O H     Me   Me     CH 207-209             II-34                                                                             Me      F           H          O H     OMe  Me     N  178-180             II-35                                                                             Me      F           H          O H     OMe  Me     CH 185-187             II-36                                                                             Me      H           5-Cl       O H     OMe  OMe    CH 215-216             II-37                                                                             Me      H           5-Cl       O H     Me   Me     CH 192-194             II-38                                                                             Me      H           5-Cl       O H     OMe  Me     N  176-178             II-39                                                                             Me      H           6-Cl       O H     OMe  OMe    CH 210-212             II-40                                                                             Me      H           6-Cl       O H     Me   Me     CH 217-220             II-41                                                                             Me      H           6-Cl       O H     OMe  Me     N  181-183             II-42                                                                             Me      H           7-Cl       O H     OMe  OMe    CH 223-225             II-43                                                                             Me      H           7-Cl       O H     OMe  Me     N  167-169             II-44                                                                             Me      Cl          H          S H     OMe  OMe    CH                     II-45                                                                             Me      Cl          H          O Me    OMe  OMe    CH                     II-46                                                                             Me      COH         H          O H     OMe  OMe    CH                     II-47                                                                             Me      COMe        H          O H     OMe  OMe    CH                     II-48                                                                             Me      COEt        H          O H     OMe  OMe    CH                     II-49                                                                             Me      COPh        H          O H     OMe  OMe    CH                     II-50                                                                             Me      COCH.sub.2 CHCH.sub.2                                                                     H          O H     OMe  OMe    CH                     II-51                                                                             Me      COCH.sub.2 CCH                                                                            H          O H     OMe  OMe    CH                     II-52                                                                             Me      COBn        H          O H     OMe  OMe    CH                     II-53                                                                             Me      NO.sub.2    H          O H     OMe  OMe    CH 155-157             II-54                                                                             Me      NH.sub.2    H          O H     OMe  OMe    CH                     II-55                                                                             Me      NHMe        H          O H     OMe  OMe    CH 143-144             II-56                                                                             Me      NMe.sub.2   H          O H     OMe  OMe    CH 183-185             II-57                                                                             Me      NHCOMe      H          O H     OMe  OMe    CH                     II-58                                                                             Me      NHCOPh      H          O H     OMe  OMe    CH                     II-59                                                                             Me      NHCOCH.sub.2 Cl                                                                           H          O H     OMe  OMe    CH                     II-60                                                                             Me      NHSO.sub.2 CH.sub.3                                                                       H          O H     OMe  OMe    CH                     II-61                                                                             Me      NHSO.sub.2 Ph                                                                             H          O H     OMe  OMe    CH                     II-62                                                                             Me      CO.sub.2 H  H          O H     OMe  OMe    CH                     II-63                                                                             Me      CO.sub.2 Me H          O H     OMe  OMe    CH 179-181             II-64                                                                             Me      CO.sub.2 Et H          O H     OMe  OMe    CH 181-182             II-65                                                                             Me      CO.sub.2 Pr H          O H     OMe  OMe    CH 188-190             II-66                                                                             Me      CO.sub.2 Pr-i                                                                             H          O H     OMe  OMe    CH 200-202             II-67                                                                             Me      CO.sub.2 Bu H          O H     OMe  OMe    CH 189-190             II-68                                                                             Me      CO.sub.2 Pen                                                                              H          O H     OMe  OMe    CH                     II-69                                                                             Me      CO.sub.2 Bn H          O H     OMe  OMe    CH                     II-70                                                                             Me      CO.sub.2 Ph H          O H     OMe  OMe    CH                     II-71                                                                             Me      CO.sub.2 CH.sub.2 CH.sub.2 F                                                              H          O H     OMe  OMe    CH                     II-72                                                                             Me      CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H          O H     OMe  OMe    CH                     II-73                                                                             Me      CO.sub.2 CH.sub.2 CCH                                                                     H          O H     OMe  OMe    CH                     II-74                                                                             Me      CO.sub.2 Me H          O H     OCHF.sub.2                                                                         OCHF.sub.2                                                                           CH                     II-75                                                                             Me      CO.sub.2 Et H          O H     OCHF.sub.2                                                                         OCHF.sub.2                                                                           CH                     II-76                                                                             Me      CO.sub.2 Me H          O H     OMe  Cl     CH                     II-77                                                                             Me      CO.sub.2 Me H          O H     OMe  Me     CH                     II-78                                                                             Me      CO.sub.2 Me H          O H     OMe  Me     N                      II-79                                                                             Me      CO.sub.2 Et H          O H     OMe  Me     N                      II-80                                                                             Me      CO.sub.2 Me H          O H     OMe  OCHF.sub.2                                                                           CH                     II-81                                                                             Me      CO.sub.2 Me 5-F        O H     OMe  OMe    CH                     II-82                                                                             Et      CO.sub.2 Me H          O H     OMe  OMe    CH 147-148             II-83                                                                             Bu      CO.sub.2 Me H          O H     OMe  OMe    CH                     II-84                                                                             Bn      CO.sub.2 Me H          O H     OMe  OMe    CH                     II-85                                                                             Ph      CO.sub.2 Me H          O H     OMe  OMe    CH                     II-86                                                                             H       CO.sub.2 Et H          O H     OMe  OMe    CH                     II-87                                                                             Me      CO.sub.2 Me H          S H     OMe  OMe    CH                     II-88                                                                             Me      CO.sub.2 Et H          S H     OMe  OMe    CH                     II-89                                                                             Me      CO.sub.2 Me H          O Me    OMe  OMe    CH                     II-90                                                                             Me      OH          H          O H     OMe  OMe    CH 179-181             II-91                                                                             Me      OMe         H          O H     OMe  OMe    CH 162-165             II-92                                                                             Me      OEt         H          O H     OMe  OMe    CH 153-154             II-93                                                                             Me      OPr         H          O H     OMe  OMe    CH 119-120             II-94                                                                             Me      OPr-i       H          O H     OMe  OMe    CH 176-179             II-95                                                                             Me      OBu         H          O H     OMe  OMe    CH 184-186             II-96                                                                             Me      OBn         H          O H     OMe  OMe    CH 200-203             II-97                                                                             Me      OBn(4-Cl)   H          O H     OMe  OMe    CH                     II-98                                                                             Me      OBn(3-OMe)  H          O H     OMe  OMe    CH                     II-99                                                                             Me      OBn(2-Me)   H          O H     OMe  OMe    CH                     II-100                                                                            Me      OPh         H          O H     OMe  OMe    CH                     II-101                                                                            Me      OPh(4-Cl)   H          O H     OMe  OMe    CH                     II-102                                                                            Me      OPh(3-OMe)  H          O H     OMe  OMe    CH                     II-103                                                                            Me      OPh(2-Me)   H          O H     OMe  OMe    CH                     II-104                                                                            Me      OCH.sub.2 CHCH.sub.2                                                                      H          O H     OMe  OMe    CH 133-136             II-105                                                                            Me      OCH.sub.2 CCH                                                                             H          O H     OMe  OMe    CH 182-183             II-106                                                                            Me      OCH.sub.2 CF.sub.3                                                                        H          O H     OMe  OMe    CH 165-170             II-107                                                                            Me      OCH.sub.2 CH.sub.2 OMe                                                                    H          O H     OMe  OMe    CH 139-141             II-108                                                                            Me      OCH.sub.2 CH.sub.2 OPh                                                                    H          O H     OMe  OMe    CH                     II-109                                                                            Me      OCOMe       H          O H     OMe  OMe    CH                     II-110                                                                            Me      OMe         H          O H     OMe  Me     CH 206-208             II-111                                                                            Me      OMe         H          O H     OMe  Me     N  198-201             II-112                                                                            Me      OMe         H          O H     Me   Me     CH 193-196             II-113                                                                            Me      OEt         H          O H     OMe  Me     N  179-181             II-114                                                                            Me      OEt         H          O H     OMe  Me     CH 174-175             II-115                                                                            Me      OEt         H          O H     Me   Me     CH 182-183             II-116                                                                            Me      CONH.sub.2  H          O H     OMe  OMe    CH                     II-117                                                                            Me      CONHMe      H          O H     OMe  OMe    CH                     II-118                                                                            Me      CONHEt      H          O H     OMe  OMe    CH                     II-119                                                                            Me      CONHPr      H          O H     OMe  OMe    CH                     II-120                                                                            Me      CONMe.sub.2 H          O H     OMe  OMe    CH 150-151             II-121                                                                            Me      CONEt.sub.2 H          O H     OMe  OMe    CH                     II-122                                                                            Me      CONHBn      H          O H     OMe  OMe    CH                     II-123                                                                            Me      CONHPh      H          O H     OMe  OMe    CH                     II-124                                                                            Me      CONHCH.sub.2 CHCH.sub.2                                                                   H          O H     OMe  OMe    CH                     II-125                                                                            Me      CONHCH.sub.2 CCH                                                                          H          O H     OMe  OMe    CH                     II-126                                                                            Me      CONHOMe     H          O H     OMe  OMe    CH                     II-127                                                                            Me      H           5-F        O H     OMe  OMe    CH 205-208             II-128                                                                            Me      H           5-F        O H     Me   Me     CH 203-206             II-129                                                                            Me      H           5-F        O H     OMe  Me     CH 186-189             II-130                                                                            Me      H           5-F        O H     OMe  Me     N  175-179             II-131                                                                            H       COOMe       H          O H     OMe  OMe    CH 179-180             II-132                                                                            H       COOMe       H          O H     OMe  Cl     CH 193-194             II-133                                                                            H       Cl          H          O H     OMe  Cl     CH 178-181             II-134                                                                            Me      Cl          H          O H     OMe  OMe    CH 171-172             II-135                                                                            Me      SO.sub.2 NH.sub.2                                                                         H          O H     OMe  OMe    CH                     II-136                                                                            H       Br          H          O H     OMe  OMe    CH 190-193             II-137                                                                            Me      H           5-OMe      O H     OMe  OMe    CH 178-181             II-138                                                                            Me      H           5-OEt      O H     OMe  OMe    CH 188-189             II-139                                                                            Me      H           5-OPr      O H     OMe  OMe    CH 197-198             II-140                                                                            Me      OCH(CF.sub.3)Me                                                                           H          O H     OMe  OMe    CH 129-130             II-141                                                                            Me      OCH.sub.2 CH.sub.2 Cl                                                                     H          O H     OMe  OMe    CH 182-186             II-142                                                                            Me      OCH.sub.2 CH.sub.2 F                                                                      H          O H     OMe  OMe    CH 162-165             II-143                                                                            Me      OCH.sub.2 CH.sub.2 OEt                                                                    H          O H     OMe  OMe    CH 138-139             II-144                                                                            Me      OCH.sub.2 CH.sub.2 OPr-i                                                                  H          O H     OMe  OMe    CH 185-187             II-145                                                                            Me      OCH.sub.2 CH.sub.2 OBu                                                                    H          O H     OMe  OMe    CH 120-121             II-146                                                                            Me      OCH.sub.2 CH.sub.2 OBu-t                                                                  H          O H     OMe  OMe    CH 169-171             II-147                                                                            Me      OCH.sub.2 COOEt                                                                           H          O H     OMe  OMe    CH 163-165             II-148                                                                            Me      OCH.sub.2 CH.sub.2 NMe.sub.2                                                              H          O H     OMe  OMe    CH 126-129             II-149                                                                            Me      SBu         H          O H     OMe  OMe    CH 156-158             II-150                                                                            Me      SPr-i       H          O H     OMe  OMe    CH 183-184             II-151                                                                            Me      SO.sub.2 Pr H          O H     OMe  OMe    CH 202-204             II-152                                                                            Me      SO.sub.2 Bu H          O H     OMe  OMe    CH 201-203             II-153                                                                            Me      SO.sub.2 Pr-i                                                                             H          O H     OMe  OMe    CH 185-187             II-154                                                                            Me      NHBn        H          O H     OMe  OMe    CH 167-168             II-155                                                                            Me      NEt.sub.2   H          O H     OMe  OMe    CH 173-175             II-156                                                                            Me      OMe         5-Cl       O H     OMe  OMe    CH 211-212             II-157                                                                            Me      Br          H          O H     OMe  Me     CH 187-189             II-158                                                                            Et      Cl          H          O H     OMe  Me     CH 205-206             II-159                                                                            Ph      Cl          H          O H     OMe  Me     CH 215-217             II-160                                                                            Me      OPr         H          O H     OMe  Me     CH 174-175             II-161                                                                            Me      OBu         H          O H     OMe  Me     CH 169-171             II-162                                                                            Me      OPr-i       H          O H     OMe  Me     CH 157-159             II-163                                                                            Me      H           5-OMe      O H     OMe  Me     CH 206-208             II-164                                                                            Me      H           5-OEt      O H     OMe  Me     CH 174-176             II-165                                                                            Me      H           5-OPr      O H     OMe  Me     CH 176-178             II-166                                                                            Me      OCH.sub.2 CF.sub.3                                                                        H          O H     OMe  Me     CH 150-153             II-167                                                                            Me      OCH(CF.sub.3)Me                                                                           H          O H     OMe  Me     CH 112-114             II-168                                                                            Me      OCH.sub.2 CH.sub.2 OMe                                                                    H          O H     OMe  Me     CH 138-139             II-169                                                                            Me      OCH.sub.2 CH.sub.2 OEt                                                                    H          O H     OMe  Me     CH 160-163             II-170                                                                            Me      OCH.sub.2 CH.sub.2 OPr-i                                                                  H          O H     OMe  Me     CH 130-132             II-171                                                                            Me      OCH.sub.2 CH.sub.2 OBu                                                                    H          O H     OMe  Me     CH 104-106             II-172                                                                            Me      OCH.sub.2 CH.sub.2 OBu-t                                                                  H          O H     OMe  Me     CH 148-149             II-173                                                                            Me      OCH.sub.2 CH.sub.2 NMe.sub.2                                                              H          O H     OMe  Me     CH 126-129             II-174                                                                            Me      SPr         H          O H     OMe  Me     CH 164-165             II-175                                                                            Me      CO.sub.2 Pr H          O H     OMe  Me     CH 179-181             II-176                                                                            Me      CO.sub.2 Pr-i                                                                             H          O H     OMe  Me     CH 187-190             II-177                                                                            Me      CO.sub.2 Bu H          O H     OMe  Me     CH 189-192             II-178                                                                            Me      NO.sub.2    H          O H     OMe  Me     CH 161-163             II-179                                                                            Me      CN          H          O H     OMe  Me     CH 195-197             II-180                                                                            Me      Br          H          O H     OMe  Me     N  172-174             II-181                                                                            Et      Cl          H          O H     OMe  Me     N  192-194             II-182                                                                            Me      OPr         H          O H     OMe  Me     N  176-177             II-183                                                                            Me      OBu         H          O H     OMe  Me     N  143-145             II-184                                                                            Me      OPr-i       H          O H     OMe  Me     N  155-156             II-185                                                                            Me      H           5-OMe      O H     OMe  Me     N  171-174             II-186                                                                            Me      H           5-OEt      O H     OMe  Me     N  180-182             II-187                                                                            Me      H           5-OPr      O H     OMe  Me     N  168-170             II-188                                                                            Me      OCH.sub.2 CF.sub.3                                                                        H          O H     OMe  Me     N  168-170             II-189                                                                            Me      OCH.sub.2 CH.sub.2 OEt                                                                    H          O H     OMe  Me     N  168-70              II-190                                                                            Me      OCH.sub.2 CH.sub.2 OPr-i                                                                  H          O H     OMe  Me     N  153-155             II-191                                                                            Me      OCH.sub.2 CH.sub.2 OBu                                                                    H          O H     OMe  Me     N  121-123             II-192                                                                            Me      OCH.sub.2 CH.sub.2 OBu-t                                                                  H          O H     OMe  Me     N  161-162             II-193                                                                            Me      OCH.sub.2 CH.sub.2 NMe.sub.2                                                              H          O H     OMe  Me     N  119-121             II-194                                                                            Me      SEt         H          O H     OMe  Me     N  160-162             II-195                                                                            Me      SPr         H          O H     OMe  Me     N  129-131             II-196                                                                            Me      NMe.sub.2   H          O H     OMe  Me     N  131-133             II-197                                                                            Me      CO.sub.2 Pr-i                                                                             H          O H     OMe  Me     N  190-191             II-198                                                                            Me      CO.sub.2 Bu H          O H     OMe  Me     N  179-181             II-199                                                                            Me      CN          H          O H     OMe  Me     N  196-197             II-200                                                                            Me      OMe         5-Cl       O H     OMe  Me     N  201-203             II-201                                                                            Me      Cl          H          O H     Cl   OMe    CH 187-189             II-202                                                                            Et      Cl          H          O H     Cl   OMe    CH 206-208             II-203                                                                            Ph      Cl          H          O H     Cl   OMe    CH 202-204             II-204                                                                            Me      OMe         H          O H     Cl   OMe    CH 220-223             II-205                                                                            Me      OPr         H          O H     Cl   OMe    CH 140-141             II-206                                                                            Me      OBu         H          O H     Cl   OMe    CH 153-154             II-207                                                                            Me      H           5-OMe      O H     Cl   OMe    CH 174-177             II-208                                                                            Me      OCH.sub.2 CF.sub.3                                                                        H          O H     Cl   OMe    CH 175-179             II-209                                                                            Me      SPr         H          O H     Cl   OMe    CH 165-167             II-210                                                                            Me      SBu         H          O H     Cl   OMe    CH 156- 157            II-211                                                                            Me      SPr-i       H          O H     Cl   OMe    CH 177-179             II-212                                                                            Me      SO.sub.2 Pr-i                                                                             H          O H     Cl   OMe    CH 184-186             II-213                                                                            Me      NHBn        H          O H     Cl   OMe    CH 160-163             II-214                                                                            Me      NMe.sub.2   H          O H     Cl   OMe    CH 197-199             II-215                                                                            Et      Cl          H          O H     Me   Me     CH 229-231             II-216                                                                            Me      OPr         H          O H     Me   Me     CH 172-173             II-217                                                                            Me      OBu         H          O H     Me   Me     CH 148-149             II-218                                                                            Me      OPr-i       H          O H     Me   Me     CH 187-190             II-219                                                                            Me      NMe.sub.2   H          O H     Me   Me     CH 174-176             II-220                                                                            Me      OMe         H          O H     OMe  OMe    N  193-195             II-221                                                                            Me      H           5-OEt      O H     OMe  OMe    N  169-170             II-222                                                                            Me      H           5-OPr      O H     OMe  OMe    N  168-169             II-223                                                                            Me      OCH.sub.2 CH.sub.2 OBu                                                                    H          O H     OMe  OMe    N  132-133             II-224                                                                            Me      OCH.sub.2 CH.sub.2 OBu-t                                                                  H          O H     OMe  OMe    N  162-163             II-225                                                                            Me      NHMe        H          O H     OMe  Me     CH 164-165             II-226                                                                            Me      NHMe        H          O H     OMe  Me     N  173-175             II-227                                                                            Me      OMe         5-Cl       O H     OMe  Me     CH 222-225             II-228                                                                            Me      OMe         5-OMe      O H     OMe  OMe    CH 168-170             II-229                                                                            Me      OCHF.sub.2  H          O H     OMe  OMe    CH 179-181             II-230                                                                            Me      OCHF.sub.2  H          O H     Me   OMe    CH 195-197             II-231                                                                            Me      OCHF.sub.2  H          O H     Me   OMe    N  165-167             II-232                                                                            Me      OCH.sub.2 CHF.sub.2                                                                       H          O H     OMe  OMe    CH 178-180             II-233                                                                            Me      OCH.sub.2 CHF.sub.2                                                                       H          O H     Me   OMe    CH 180-182             II-234                                                                            Me      OCH.sub.2 CHF.sub.2                                                                       H          O H     Me   OMe    N  164-166             II-235                                                                            Me      OCH.sub.2 CH.sub.2 CF.sub.3                                                               H          O H     OMe  OMe    CH                     II-236                                                                            Me      OCH.sub.2 CH.sub.2 CF.sub.3                                                               H          O H     Me   OMe    CH                     II-237                                                                            Me      OCH.sub.2 CH.sub.2 CF.sub.3                                                               H          O H     Me   OMe    N                      II-238                                                                            Me      OCH(CF.sub.2 CF.sub.3)Me                                                                  H          O H     OMe  OMe    CH                     II-239                                                                            Me      OCH(CF.sub.2 CF.sub.3)Me                                                                  H          O H     Me   OMe    CH                     II-240                                                                            Me      OCH(CF.sub.2 CF.sub.3)Me                                                                  H          O H     Me   OMe    N                      II-241                                                                            Me      OCH.sub.2 CF.sub.2 CHF.sub.2                                                              H          O H     OMe  OMe    CH                     II-242                                                                            Me      OCH.sub.2 CF.sub.2 CHF.sub.2                                                              H          O H     Me   OMe    CH                     II-243                                                                            Me      OCH.sub.2 CF.sub.2 CHF.sub.2                                                              H          O H     Me   OMe    N                      II-244                                                                            Me      OCH.sub.2 CF.sub.2 CF.sub.3                                                               H          O H     OMe  OMe    CH                     II-245                                                                            Me      OCH.sub.2 CF.sub.2 CF.sub.3                                                               H          O H     Me   OMe    CH                     II-246                                                                            Me      OCH.sub.2 CF.sub.2 CF.sub.3                                                               H          O H     Me   OMe    N                      II-247                                                                            Me      OCH.sub.2 CHCl.sub.2                                                                      H          O H     OMe  OMe    CH                     II-248                                                                            Me      OCH.sub.2 CHCl.sub.2                                                                      H          O H     Me   OMe    CH                     II-249                                                                            Me      OCF.sub.2 CHCl.sub.2                                                                      H          O H     Me   OMe    N                      II-250                                                                            Me      OCF.sub.2 CH.sub.2 Cl                                                                     H          O H     OMe  OMe    CH                     II-251                                                                            Me      OCF.sub.2 CH.sub.2 Cl                                                                     H          O H     Me   OMe    CH                     II-252                                                                            Me      OCF.sub.2 CH.sub.2 Cl                                                                     H          O H     Me   OMe    N                      II-253                                                                            Me      OCF.sub.2 CHFCl                                                                           H          O H     OMe  OMe    CH                     II-254                                                                            Me      OCF.sub.2 CHFCl                                                                           H          O H     Me   OMe    CH                     II-255                                                                            Me      OCF.sub.3 CHFCl                                                                           H          O H     Me   OMe    N                      II-256                                                                            Me      OCF.sub.3   H          O H     OMe  OMe    CH                     II-257                                                                            Me      OCF.sub.3   H          O H     Me   OMe    CH                     II-258                                                                            Me      OCF.sub.3   H          O H     Me   OMe    N                      II-259                                                                            Me      OCH.sub.2 CHCHCl                                                                          H          O H     OMe  OMe    CH 160-162             II-260                                                                            Me      OCH.sub.2 CHCHCl                                                                          H          O H     Me   OMe    CH                     II-261                                                                            Me      OCH.sub.2 CHCHCl                                                                          H          O H     Me   OMe    N                      II-262                                                                            Me      OCH.sub.2 CHCCl.sub.2                                                                     H          O H     OMe  OMe    CH                     II-263                                                                            Me      OCH.sub.2 CHCCl.sub.2                                                                     H          O H     Me   OMe    CH                     II-264                                                                            Me      OCH.sub.2 CHCCl.sub.2                                                                     H          O H     Me   OMe    N                      II-265                                                                            Me      OCH.sub.2 C(Cl)CH.sub.2                                                                   H          O H     OMe  OMe    CH 160-162             II-266                                                                            Me      OCH.sub.2 C(Cl)CH.sub.2                                                                   H          O H     Me   OMe    CH                     II-267                                                                            Me      OCH.sub.2 C(Cl)CH.sub.2                                                                   H          O H     Me   OMe    N                      II-268                                                                            Me      OCH.sub.2 C(Me)CH.sub.2                                                                   H          O H     OMe  OMe    CH 163-164             II-269                                                                            Me      OCH.sub.2 C(Me)CH.sub.2                                                                   H          O H     Me   OMe    CH                     II-270                                                                            Me      OCH.sub.2 C(Me)CH.sub.2                                                                   H          O H     Me   OMe    N                      II-271                                                                            Me      OCH.sub.2 CHCHMe                                                                          H          O H     OMe  OMe    CH                     II-272                                                                            Me      OCH.sub.2 CHCHMe                                                                          H          O H     Me   OMe    CH                     II-273                                                                            Me      OCH.sub.2 CHCHMe                                                                          H          O H     Me   OMe    N                      II-274                                                                            Me      OCH.sub.2 CH.sub.2 N.sub.3                                                                H          O H     OMe  OMe    CH                     II-275                                                                            Me      OCH.sub.2 CH.sub.2 N.sub.3                                                                H          O H     Me   OMe    CH                     II-276                                                                            Me      OCH.sub.2 CH.sub.2 N.sub.3                                                                H          O H     Me   OMe    N                      II-277                                                                            Me      OCH.sub.2 OMe                                                                             H          O H     OMe  OMe    CH 165-167             II-278                                                                            Me      OCH.sub.2 OMe                                                                             H          O H     Me   OMe    CH                     II-279                                                                            Me      OCH.sub.2 OMe                                                                             H          O H     Me   OMe    N                      II-280                                                                            Me      OCH.sub.2 OEt                                                                             H          O H     OMe  OMe    CH 154-155             II-281                                                                            Me      OCH.sub.2 OEt                                                                             H          O H     Me   OMe    CH                     II-282                                                                            Me      OCH.sub.2 OEt                                                                             H          O H     Me   OMe    N                      II-283                                                                            Me      OCH.sub.2 OBn                                                                             H          O H     OMe  OMe    CH 162-164             II-284                                                                            Me      OCH.sub.2 OBn                                                                             H          O H     Me   OMe    CH                     II-285                                                                            Me      OCH.sub.2 OBn                                                                             H          O H     Me   OMe    N                      II-286                                                                            Me      OCH.sub.2 OCH.sub.2 CF.sub.3                                                              H          O H     OMe  OMe    CH                     II-287                                                                            Me      OCH.sub.2 OCH.sub.2 CF.sub.3                                                              H          O H     Me   OMe    CH                     II-288                                                                            Me      OCH.sub.2 OCH.sub.2 CF.sub.3                                                              H          O H     Me   OMe    N                      II-289                                                                            Me      OCH.sub.2 OBu-t                                                                           H          O H     OMe  OMe    CH                     II-290                                                                            Me      OCH.sub.2 OBu-t                                                                           H          O H     Me   OMe    CH                     II-291                                                                            Me      OCH.sub.2 OBu-t                                                                           H          O H     Me   OMe    N                      II-292                                                                            Me      OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                          H          O H     OMe  OMe    CH                     II-293                                                                            Me      OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                          H          O H     Me   OMe    CH                     II-294                                                                            Me      OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                          H          O H     Me   OMe    N                      II-295                                                                            Me      OCH.sub.2 CN                                                                              H          O H     OMe  OMe    CH                     II-296                                                                            Me      OCH.sub.2 CN                                                                              H          O H     Me   OMe    CH                     II-297                                                                            Me      OCH.sub.2 CN                                                                              H          O H     Me   OMe    N                      II-298                                                                            Me      OCH.sub.2 COOMe                                                                           H          O H     OMe  OMe    CH                     II-299                                                                            Me      OCH.sub.2 COOMe                                                                           H          O H     Me   OMe    CH                     II-300                                                                            Me      OCH.sub.2 COOMe                                                                           H          O H     Me   OMe    N                      II-301                                                                            Me      OCH.sub.2 COOPr                                                                           H          O H     OMe  OMe    CH                     II-302                                                                            Me      OCH.sub.2 COOPr                                                                           H          O H     Me   OMe    CH                     II-303                                                                            Me      OCH.sub.2 COOPr                                                                           H          O H     Me   OMe    N                      II-304                                                                            Me      OCH.sub.2 COOPr-i                                                                         H          O H     OMe  OMe    CH                     II-305                                                                            Me      OCH.sub.2 COOPr-i                                                                         H          O H     Me   OMe    CH                     II-306                                                                            Me      OCH.sub.2 COOPr-i                                                                         H          O H     Me   OMe    N                      II-307                                                                            Me      OCH.sub.2 SMe                                                                             H          O H     OMe  OMe    CH                     II-308                                                                            Me      OCH.sub.2 SMe                                                                             H          O H     Me   OMe    CH                     II-309                                                                            Me      OCH.sub.2 SMe                                                                             H          O H     Me   OMe    N                      II-310                                                                            Me      OCH.sub.2 CH.sub.2 SMe                                                                    H          O H     OMe  OMe    CH                     II-311                                                                            Me      OCH.sub.2 CH.sub.2 SMe                                                                    H          O H     Me   OMe    CH                     II-312                                                                            Me      OCH.sub.2 CH.sub.2 SMe                                                                    H          O H     Me   OMe    N                      II-313                                                                            Me      SCF.sub.3   H          O H     OMe  OMe    CH                     II-314                                                                            Me      SCF.sub.3   H          O H     Me   OMe    CH                     II-315                                                                            Me      SCF.sub.3   H          O H     Me   OMe    N                      II-316                                                                            Me      SCH.sub.2 CH.sub.2 Cl                                                                     H          O H     OMe  OMe    CH                     II-317                                                                            Me      SCH.sub.2 CH.sub.2 Cl                                                                     H          O H     Me   OMe    CH                     II-318                                                                            Me      SCH.sub.2 CH.sub.2 Cl                                                                     H          O H     Me   OMe    N                      II-319                                                                            Me      SCH.sub.2 CH.sub.2 F                                                                      H          O H     OMe  OMe    CH                     II-320                                                                            Me      SCH.sub.2 CH.sub.2 F                                                                      H          O H     Me   OMe    CH                     II-321                                                                            Me      SCH.sub.2 CH.sub.2 F                                                                      H          O H     Me   OMe    N                      II-322                                                                            Me      SOEt        H          O H     OMe  OMe    CH                     II-323                                                                            Me      SOEt        H          O H     Me   OMe    CH                     II-324                                                                            Me      SOEt        H          O H     Me   OMe    N                      II-325                                                                            Me      SO.sub.2 NHOEt                                                                            H          O H     OMe  OMe    CH                     II-326                                                                            Me      SO.sub.2 NHOEt                                                                            H          O H     Me   OMe    CH                     II-327                                                                            Me      SO.sub.2 NHOEt                                                                            H          O H     Me   OMe    N                      II-328                                                                            Me      SO.sub.2 CH.sub.2 CHCH.sub.2                                                              H          O H     OMe  OMe    CH                     II-329                                                                            Me      SO.sub.2 CH.sub.2 CHCH.sub.2                                                              H          O H     Me   OMe    CH                     II-330                                                                            Me      SO.sub.2 CH.sub.2 CHCH.sub.2                                                              H          O H     Me   OMe    N                      II-331                                                                            Me      SO.sub.2 NEt.sub.2                                                                        H          O H     OMe  OMe    CH                     II-332                                                                            Me      SO.sub.2 NEt.sub.2                                                                        H          O H     Me   OMe    CH                     II-333                                                                            Me      SO.sub.2 NEt.sub.2                                                                        H          O H     Me   OMe    N                      II-334                                                                            Me      Et          H          O H     OMe  OMe    CH                     II-335                                                                            Me      Et          H          O H     Me   OMe    CH                     II-336                                                                            Me      Et          H          O H     Me   OMe    N                      II-337                                                                            Me      Pr          H          O H     OMe  OMe    CH                     II-338                                                                            Me      Pr          H          O H     Me   OMe    CH                     II-339                                                                            Me      Pr          H          O H     Me   OMe    N                      II-340                                                                            Me      Pr-i        H          O H     OMe  OMe    CH                     II-341                                                                            Me      Pr-i        H          O H     Me   OMe    CH                     II-342                                                                            Me      Pr-i        H          O H     Me   OMe    N                      II-343                                                                            Me      Bu          H          O H     OMe  OMe    CH                     II-344                                                                            Me      Bu          H          O H     Me   OMe    CH                     II-345                                                                            Me      Bu          H          O H     Me   OMe    N                      II-346                                                                            Me      Bu-t        H          O H     OMe  OMe    CH                     II-347                                                                            Me      Bu-t        H          O H     Me   OMe    CH                     II-348                                                                            Me      Bu-t        H          O H     Me   OMe    N                      II-349                                                                            Me      CH.sub.2 Cl H          O H     OMe  OMe    CH                     II-350                                                                            Me      CH.sub.2 Cl H          O H     Me   OMe    CH                     II-351                                                                            Me      CH.sub.2 Cl H          O H     Me   OMe    N                      II-352                                                                            Me      CH.sub.2 F  H          O H     OMe  OMe    CH                     II-353                                                                            Me      CH.sub.2 F  H          O H     Me   OMe    CH                     II-354                                                                            Me      CH.sub.2 F  H          O H     Me   OMe    N                      II-355                                                                            Me      CH.sub.2 OMe                                                                              H          O H     OMe  OMe    CH                     II-356                                                                            Me      CH.sub.2 OMe                                                                              H          O H     Me   OMe    CH                     II-357                                                                            Me      CH.sub.2 OMe                                                                              H          O H     Me   OMe    N                      II-358                                                                            Me      CH.sub.2 CF.sub.3                                                                         H          O H     OMe  OMe    CH                     II-359                                                                            Me      CH.sub.2 CF.sub.3                                                                         H          O H     Me   OMe    CH                     II-360                                                                            Me      CH.sub.2 CF.sub.3                                                                         H          O H     Me   OMe    N                      II-361                                                                            Me                                                                                     ##STR44##  H          O H     OMe  OMe    CH                     II-362                                                                            Me                                                                                     ##STR45##  H          O H     Me   OMe    CH                     II-363                                                                            Me                                                                                     ##STR46##  H          O H     Me   OMe    N                      II-364                                                                            Me      CH.sub.2 CH.sub.2 CF.sub.3                                                                H          O H     OMe  OMe    CH                     II-365                                                                            Me      CH.sub.2 CH.sub.2 CF.sub.3                                                                H          O H     Me   OMe    CH                     II-366                                                                            Me      CH.sub.2 CH.sub.2 CF.sub.3                                                                H          O H     Me   OMe    N                      II-367                                                                            Me      CH.sub.2 CHCH.sub.2                                                                       H          O H     OMe  OMe    CH                     II-368                                                                            Me      CH.sub.2 CHCH.sub.2                                                                       H          O H     Me   OMe    CH                     II-369                                                                            Me      CH.sub.2 CHCH.sub.2                                                                       H          O H     Me   OMe    N                      II-370                                                                            Me      CH.sub.2 CCH                                                                              H          O H     OMe  OMe    CH                     II-371                                                                            Me      CH.sub.2 CCH                                                                              H          O H     Me   OMe    CH                     II-372                                                                            Me      CH.sub.2 CCH                                                                              H          O H     Me   OMe    N                      II-373                                                                            Me      CH.sub.2 COOMe                                                                            H          O H     OMe  OMe    CH                     II-374                                                                            Me      CH.sub.2 COOMe                                                                            H          O H     Me   OMe    CH                     II-375                                                                            Me      CH.sub.2 COOMe                                                                            H          O H     Me   OMe    N                      II-376                                                                            Me      CH.sub.2 COOEt                                                                            H          O H     OMe  OMe    CH                     II-377                                                                            Me      CH.sub.2 COOEt                                                                            H          O H     Me   OMe    CH                     II-378                                                                            Me      CH.sub.2 COOEt                                                                            H          O H     Me   OMe    N                      II-379                                                                            Me      CH.sub.2 CN H          O H     OMe  OMe    CH                     II-380                                                                            Me      CH.sub.2 CN H          O H     Me   OMe    CH                     II-381                                                                            Me      CH.sub.2 CN H          O H     Me   OMe    N                      II-382                                                                            Me      CH.sub.2 CONMe.sub.2                                                                      H          O H     OMe  OMe    CH                     II-383                                                                            Me      CH.sub.2 CONMe.sub.2                                                                      H          O H     Me   OMe    CH                     II-384                                                                            Me      CH.sub.2 CONMe.sub.2                                                                      H          O H     Me   OMe    N                      II-385                                                                            Me      CH.sub.2 SO.sub.2 NMe.sub.2                                                               H          O H     OMe  OMe    CH                     II-386                                                                            Me      CH.sub.2 SO.sub.2 NMe.sub.2                                                               H          O H     Me   OMe    CH                     II-387                                                                            Me      CH.sub.2 SO.sub.2 NMe.sub.2                                                               H          O H     Me   OMe    N                      II-388                                                                            Me      CH.sub.2 NMe.sub.2                                                                        H          O H     OMe  OMe    CH                     II-389                                                                            Me      CH.sub.2 NMe.sub.2                                                                        H          O H     Me   OMe    CH                     II-390                                                                            Me      CH.sub.2 NMe.sub.2                                                                        H          O H     Me   OMe    N                      II-391                                                                            Me      CHCH.sub.2  H          O H     OMe  OMe    CH                     II-392                                                                            Me      CHCH.sub.2  H          O H     Me   OMe    CH                     II-393                                                                            Me      CHCH.sub.2  H          O H     Me   OMe    N                      II-394                                                                            Me      CHCHMe      H          O H     OMe  OMe    CH                     II-395                                                                            Me      CHCHMe      H          O H     Me   OMe    CH                     II-396                                                                            Me      CHCHMe      H          O H     Me   OMe    N                      II-397                                                                            Me      CCH         H          O H     OMe  OMe    CH                     II-398                                                                            Me      CCH         H          O H     Me   OMe    CH                     II-399                                                                            Me      CCH         H          O H     Me   OMe    N                      II-400                                                                            Me      CCMe        H          O H     OMe  OMe    CH                     II-401                                                                            Me      CCMe        H          O H     Me   OMe    CH                     II-402                                                                            Me      CCMe        H          O H     Me   OMe    N                      II-403                                                                            Me      CHCHCOOMe   H          O H     OMe  OMe    CH                     II-404                                                                            Me      CHCHCOOMe   H          O H     Me   OMe    CH                     II-405                                                                            Me      CHCHCOOMe   H          O H     Me   OMe    N                      II-406                                                                            Me      CH(Me)COMe  H          O H     OMe  OMe    CH                     II-407                                                                            Me      CH(Me)COMe  H          O H     Me   OMe    CH                     II-408                                                                            Me      CH(Me)COMe  H          O H     Me   OMe    N                      II-409                                                                            Me      CH(Me)COEt  H          O H     OMe  OMe    CH                     II-410                                                                            Me      CH(Me)COEt  H          O H     Me   OMe    CH                     II-411                                                                            Me      CH(Me)COEt  H          O H     Me   OMe    N                      II-412                                                                            Me      CH(Et)COMe  H          O H     OMe  OMe    CH                     II-413                                                                            Me      CH(Et)COMe  H          O H     Me   OMe    CH                     II-414                                                                            Me      CH(Et)COMe  H          O H     Me   OMe    N                      II-415                                                                            Me      CH(Et)COEt  H          O H     OMe  OMe    CH                     II-416                                                                            Me      CH(Et)COEt  H          O H     Me   OMe    CH                     II-417                                                                            Me      CH(Et)COEt  H          O H     Me   OMe    N                      II-418                                                                            Me                                                                                     ##STR47##  H          O H     OMe  OMe    CH                     II-419                                                                            Me                                                                                     ##STR48##  H          O H     Me   OMe    CH                     II-420                                                                            Me                                                                                     ##STR49##  H          O H     Me   OMe    N                      II-421                                                                            Me      COPr        H          O H     OMe  OMe    CH                     II-422                                                                            Me      COPr        H          O H     Me   OMe    CH                     II-423                                                                            Me      COPr        H          O H     Me   OMe    N                      II-424                                                                            Me      COPr-i      H          O H     OMe  OMe    CH                     II-425                                                                            Me      COPr-i      H          O H     Me   OMe    CH                     II-426                                                                            Me      COPr-i      H          O H     Me   OMe    N                      II-427                                                                            Me      CHNOMe      H          O H     OMe  OMe    CH                     II-428                                                                            Me      CHNOMe      H          O H     Me   OMe    CH                     II-429                                                                            Me      CHNOMe      H          O H     Me   OMe    N                      II-430                                                                            Me      CHNOEt      H          O H     OMe  OMe    CH                     II-431                                                                            Me      CHNOEt      H          O H     Me   OMe    CH                     II-432                                                                            Me      CHNOEt      H          O H     Me   OMe    N                      II-433                                                                            Me      C(Me)NOMe   H          O H     OMe  OMe    CH                     II-434                                                                            Me      C(Me)NOMe   H          O H     Me   OMe    CH                     II-435                                                                            Me      C(Me)NOMe   H          O H     Me   OMe    N                      II-436                                                                            Me      C(Me)NOEt   H          O H     OMe  OMe    CH                     II-437                                                                            Me      C(Me)NOEt   H          O H     Me   OMe    CH                     II-438                                                                            Me      C(Me)NOEt   H          O H     Me   OMe    N                      II-439                                                                            Me      C(Me)NOPr   H          O H     OMe  OMe    CH                     II-440                                                                            Me      C(Me)NOPr   H          O H     Me   OMe    CH                     II-441                                                                            Me      C(Me)NOPr   H          O H     Me   OMe    N                      II-442                                                                            Me      C(Me)NOCH.sub.2 CH.sub.2 Cl                                                               H          O H     OMe  OMe    CH                     II-443                                                                            Me      C(Me)NOCH.sub.2 CH.sub.2 Cl                                                               H          O H     Me   OMe    CH                     II-444                                                                            Me      C(Me)NOCH.sub.2 CH.sub.2 Cl                                                               H          O H     Me   OMe    N                      II-445                                                                            Me      C(Me)NOCH.sub.2 CH.sub.2 F                                                                H          O H     OMe  OMe    CH                     II-446                                                                            Me      C(Me)NOCH.sub.2 CH.sub.2 F                                                                H          O H     Me   OMe    CH                     II-447                                                                            Me      C(Me)NOCH.sub.2 CH.sub.2 F                                                                H          O H     Me   OMe    N                      II-448                                                                            Me      NHEt        H          O H     OMe  OMe    CH                     II-449                                                                            Me      NHEt        H          O H     Me   OMe    CH                     II-450                                                                            Me      NHEt        H          O H     Me   OMe    N                      II-451                                                                            Me      NHPr        H          O H     OMe  OMe    CH                     II-452                                                                            Me      NHPr        H          O H     Me   OMe    CH                     II-453                                                                            Me      NHPr        H          O H     Me   OMe    N                      II-454                                                                            Me      NHCOOMe     H          O H     OMe  OMe    CH                     II-455                                                                            Me      NHCOOMe     H          O H     Me   OMe    CH                     II-456                                                                            Me      NHCOOMe     H          O H     Me   OMe    N                      II-457                                                                            Me      NHCOOEt     H          O H     OMe  OMe    CH                     II-458                                                                            Me      NHCOOEt     H          O H     Me   OMe    CH                     II-459                                                                            Me      NHCOOEt     H          O H     Me   OMe    N                      II-460                                                                            Me      NHCOOPh     H          O H     OMe  OMe    CH                     II-461                                                                            Me      NHCOOPh     H          O H     Me   OMe    CH                     II-462                                                                            Me      NHCOOPh     H          O H     Me   OMe    N                      II-463                                                                            Me      N(Me)SO.sub.2 Me                                                                          H          O H     OMe  OMe    CH                     II-464                                                                            Me      N(Me)SO.sub.2 Me                                                                          H          O H     Me   OMe    CH                     II-465                                                                            Me      N(Me)SO.sub.2 Me                                                                          H          O H     Me   OMe    N                      II-466                                                                            Me      N(Et)SO.sub.2 Me                                                                          H          O H     OMe  OMe    CH                     II-467                                                                            Me      N(Et)SO.sub.2 Me                                                                          H          O H     Me   OMe    CH                     II-468                                                                            Me      N(Et)SO.sub.2 Me                                                                          H          O H     Me   OMe    N                      II-469                                                                            Me      N(Me)SO.sub.2 Et                                                                          H          O H     OMe  OMe    CH                     II-470                                                                            Me      N(Me)SO.sub.2 Et                                                                          H          O H     Me   OMe    CH                     II-471                                                                            Me      N(Me)SO.sub.2 Et                                                                          H          O H     Me   OMe    N                      II-472                                                                            Me      N(Et)SO.sub.2 Et                                                                          H          O H     OMe  OMe    CH                     II-473                                                                            Me      N(Et)SO.sub.2 Et                                                                          H          O H     Me   OMe    CH                     II-474                                                                            Me      N(Et)SO.sub.2 Et                                                                          H          O H     Me   OMe    N                      II-475                                                                            Me      NHCOEt      H          O H     OMe  OMe    CH                     II-476                                                                            Me      NHCOEt      H          O H     Me   OMe    CH                     II-477                                                                            Me      NHCOEt      H          O H     Me   OMe    N                      II-478                                                                            Me      NHCOCF.sub.3                                                                              H          O H     OMe  OMe    CH                     II-479                                                                            Me      NHCOCF.sub.3                                                                              H          O H     Me   OMe    CH                     II-480                                                                            Me      NHCOCF.sub.3                                                                              H          O H     Me   OMe    N                      II-481                                                                            Me      NCHMe       H          O H     OMe  OMe    CH                     II-482                                                                            Me      NCHMe       H          O H     Me   OMe    CH                     II-483                                                                            Me      NCHMe       H          O H     Me   OMe    N                      II-484                                                                            Me      NCH-Ph      H          O H     OMe  OMe    CH                     II-485                                                                            Me      NCH-Ph      H          O H     Me   OMe    CH                     II-486                                                                            Me      NCH-Ph      H          O H     Me   OMe    N                      II-487                                                                            Me      N.sub.3     H          O H     OMe  OMe    CH                     II-488                                                                            Me      N.sub.3     H          O H     Me   OMe    CH                     II-489                                                                            Me      N.sub.3     H          O H     Me   OMe    N                      II-490                                                                            Me      I           H          O H     OMe  OMe    CH                     II-491                                                                            Me      I           H          O H     Me   OMe    CH                     II-492                                                                            Me      I           H          O H     Me   OMe    N                      II-493                                                                            Me      OCOEt       H          O H     OMe  OMe    CH                     II-494                                                                            Me      OCOEt       H          O H     Me   OMe    CH                     II-495                                                                            Me      OCOEt       H          O H     Me   OMe    N                      II-496                                                                            Me      OCOPr       H          O H     OMe  OMe    CH                     II-497                                                                            Me      OCOPr       H          O H     Me   OMe    CH                     II-498                                                                            Me      OCOPr       H          O H     Me   OMe    N                      II-499                                                                            Me      OCOPh       H          O H     OMe  OMe    CH                     II-500                                                                            Me      OCOPh       H          O H     Me   OMe    CH                     II-501                                                                            Me      OCOPh       H          O H     Me   OMe    N                      II-502                                                                            Me      OCONMe.sub.2                                                                              H          O H     OMe  OMe    CH                     II-503                                                                            Me      OCONMe.sub.2                                                                              H          O H     Me   OMe    CH                     II-504                                                                            Me      OCONMe.sub.2                                                                              H          O H     Me   OMe    N                      II-505                                                                            Me      Cl          H          O H     CF.sub.3                                                                           OMe    CH                     II-506                                                                            Me      OPr-i       H          O H     Cl   OMe    CH                     II-507                                                                            Me      SEt         H          O H     Me   OMe    CH                     II-508                                                                            Me      SEt         H          O H     Cl   OMe    CH                     II-509                                                                            Me      SEt         H          O H     Me   Me     CH                     II-510                                                                            Me      SEt         H          O H     OMe  OMe    N                      II-511                                                                            Me      SBu         H          O H     OMe  Me     CH                     II-512                                                                            Me      SBu         H          O H     OMe  Me     N                      II-513                                                                            Me      SPr-i       H          O H     OMe  Me     CH                     II-514                                                                            Me      SPr-i       H          O H     OMe  Me     N                      II-515                                                                            Me      SOEt        H          O H     OMe  OMe    N                      II-516                                                                            Me      SO.sub.2 Et H          O H     OMe  Me     CH                     II-517                                                                            Me      SO.sub.2 Et H          O H     OMe  Me     N                      II-518                                                                            Me      SO.sub.2 Et H          O H     OMe  Cl     CH                     II-519                                                                            Me      SO.sub.2 Pr H          O H     OMe  Me     CH                     II-520                                                                            Me      SO.sub.2 Pr H          O H     OMe  Me     N                      II-521                                                                            Me      SO.sub.2 Pr H          O H     OMe  Cl     CH                     II-522                                                                            Me      SO.sub.2 Bu H          O H     OMe  Me     CH                     II-523                                                                            Me      SO.sub.2 Bu H          O H     OMe  Me     N                      II-524                                                                            Me      SO.sub.2 Bu H          O H     OMe  Cl     CH                     II-525                                                                            Me      SO.sub.2 Pr-i                                                                             H          O H     OMe  Me     CH                     II-526                                                                            Me      SO.sub.2 Pr-i                                                                             H          O H     OMe  Me     N                      II-527                                                                            Me      COOPr       H          O H     OMe  Me     N                      II-528                                                                            Me      NO.sub.2    H          O H     OMe  Cl     CH                     II-529                                                                            Me      CONMe.sub.2 H          O H     OMe  Me     CH                     II-530                                                                            Me      Br          H          O H     OMe  Cl     CH                     II-531                                                                            Me                                                                                     ##STR50##  H          O H     OMe  OMe    CH 156-158             II-532                                                                            Me      OCH.sub.2 -Bu-t                                                                           H          O H     OMe  OMe    CH 144-146             II-533                                                                            Me      OCH.sub.2 -Bu-t                                                                           H          O H     Me   OMe    CH 126-128             II-534                                                                            Me      OCH.sub.2 CHCMe.sub.2                                                                     H          O H     OMe  OMe    CH 164-166             II-535                                                                            Me      OCH.sub.2 CH.sub.2 CH.sub.2 F                                                             H          O H     OMe  OMe    CH 136-138             II-536                                                                            Me      OCH.sub.2 CH.sub.2 CH.sub.2 F                                                             H          O H     Me   OMe    CH 173-175             II-537                                                                            Me      OCH.sub.2 CH.sub.2 CH.sub.2 F                                                             H          O H     Me   OMe    N  160-163             II-538                                                                            Me      CH.sub.2 CH.sub.2 N.sub.3                                                                 H          O H     OMe  OMe    CH                     II-539                                                                            Me                                                                                     ##STR51##  H          O H     OMe  OMe    CH                     II-540                                                                            Me      COCF.sub.3  H          O H     OMe  OMe    CH                     II-541                                                                            Me      COOCH.sub.2 CHCHCl                                                                        H          O H     OMe  OMe    CH                     II-542                                                                            Me      SO.sub.2 CF.sub.3                                                                         H          O H     OMe  OMe    CH                     II-543                                                                            Me      OCOCF.sub.3 H          O H     OMe  OMe    CH                     II-544                                                                            Me      OCH.sub.2 OPh                                                                             H          O H     OMe  OMe    CH                     II-545                                                                            Me      CHNOH       H          O H     OMe  OMe    CH                     II-546                                                                            Me      CHNOCH.sub.2 CHCH.sub.2                                                                   H          O H     OMe  OMe    CH                     II-547                                                                            Me      CHNOCH.sub.2 CCH                                                                          H          O H     OMe  OMe    CH                     II-548                                                                            Me      C(Me)NOBn   H          O H     OMe  OMe    CH                     II-549                                                                            Me      C(Me)NOPh   H          O H     OMe  OMe    CH                     II-550                                                                            Me      C(Bn)NOMe   H          O H     OMe  OMe    CH                     II-551                                                                            Me      C(Ph)NOMe   H          O H     OMe  OMe    CH                     II-552                                                                            Me      C(CF.sub.3)NOMe                                                                           H          O H     OMe  OMe    CH                     II-553                                                                            Me      COOCH.sub.2 CH.sub.2 Cl                                                                   H          O H     OMe  OMe    CH                     II-554                                                                            Me      COOCH.sub.2 CF.sub.3                                                                      H          O H     OMe  OMe    CH                     II-555                                                                            Me      Cl          5-Cl       O H     OMe  Me     N                      II-556                                                                            Me      Cl          5-OMe      O H     OMe  OMe    CH 197-199             II-557                                                                            Me      Cl          5-F        O H     OMe  OMe    CH                     II-558                                                                            Me      F           5-Cl       O H     OMe  OMe    CH                     II-559                                                                            Me      F           5-F        O H     OMe  OMe    CH                     II-560                                                                            Me      COOMe       5-Cl       O H     OMe  OMe    CH                     II-561                                                                            Me      COOEt       5-Cl       O H     OMe  OMe    CH                     II-562                                                                            Me      COOPr       5-Cl       O H     OMe  OMe    CH                     II-563                                                                            Me      COOPr-i     5-Cl       O H     OMe  OMe    CH                     II-564                                                                            Me      OMe         5-COOMe    O H     OMe  OMe    CH                     II-565                                                                            Me      COOMe       5-OMe      O H     OMe  OMe    CH                     II-566                                                                            Me      H           5-CN       O H     OMe  OMe    CH                     II-567                                                                            Me      H           5-CF.sub.3 O H     OMe  OMe    CH                     II-568                                                                            Me      H           5-COOMe    O H     OMe  OMe    CH                     II-569                                                                            Me      H           5-COOEt    O H     OMe  OMe    CH                     II-570                                                                            Me      H           5-COOPr    O H     OMe  OMe    CH                     II-571                                                                            Me      H           5-COOPr-i  O H     OMe  OMe    CH                     II-572                                                                            Me      H           5-COOCH.sub.2 CH.sub.2 Cl                                                                O H     OMe  OMe    CH                     II-573                                                                            Me      H           5-COOCH.sub.2 CH.sub.2 F                                                                 O H     OMe  OMe    CH                     II-574                                                                            Me      H           5-COOCH.sub.2 CF.sub.3                                                                   O H     OMe  OMe    CH                     II-575                                                                            Me      H           5-COOCH.sub.2 OMe                                                                        O H     OMe  OMe    CH                     II-576                                                                            Me      H           5-CONMe.sub.2                                                                            O H     OMe  OMe    CH                     II-577                                                                            Me      H           5-OCH.sub.2 CH.sub.2 F                                                                   O H     OMe  OMe    CH                     II-578                                                                            Me      H           5-OCHF.sub.2                                                                             O H     OMe  OMe    CH                     II-579                                                                            Me      H           5-OCH.sub.2 CF.sub.3                                                                     O H     OMe  OMe    CH                     II-580                                                                            Me      H           5-OCH.sub.2 CH.sub.2 CH.sub.2 F                                                          O H     OMe  OMe    CH                     II-581                                                                            Me      H           5-OCH.sub.2 CHCH.sub.2                                                                   O H     OMe  OMe    CH                     II-582                                                                            Me      H           5-OCH.sub.2 CCH                                                                          O H     OMe  OMe    CH                     II-583                                                                            Me      H           5-NO.sub.2 O H     OMe  OMe    CH                     II-584                                                                            Me      H           5-SMe      O H     OMe  OMe    CH                     II-585                                                                            Me      H           5-SEt      O H     OMe  OMe    CH                     II-586                                                                            Me      H           5-SPr      O H     OMe  OMe    CH                     II-587                                                                            Me      H           5-SPr-i    O H     OMe  OMe    CH                     II-588                                                                            Me      H           5-SO.sub.2 Et                                                                            O H     OMe  OMe    CH                     II-589                                                                            Me      H           5-SO.sub.2 Pr                                                                            O H     OMe  OMe    CH                     II-590                                                                            Me      H           5-SO.sub.2 Pr-i                                                                          O H     OMe  OMe    CH                     II-591                                                                            Me      H           5-SOEt     O H     OMe  OMe    CH                     II-592                                                                            Me      H           5-Me       O H     OMe  OMe    CH                     II-593                                                                            Me      H           5-Et       O H     OMe  OMe    CH                     II-594                                                                            Me      H           5-Pr       O H     OMe  OMe    CH                     II-595                                                                            Me      H           5-SO.sub.2 NMe.sub.2                                                                     O H     OMe  OMe    CH                     II-596                                                                            Me      H           5-OCF.sub.3                                                                              O H     OMe  OMe    CH                     II-597                                                                            Me      H           5-CH.sub.2 CF.sub.3                                                                      O H     OMe  OMe    CH                     II-598                                                                            Me      H           5-CH.sub.2 CHCH.sub.2                                                                    O H     OMe  OMe    CH                     II-599                                                                            Me      H           5-COOMe    O H     OMe  Me     CH                     II-600                                                                            Me      H           5-COOMe    O H     OMe  Me     N                      II-601                                                                            Me      H           5-COOMe    O H     OMe  OMe    N                      II-602                                                                            Me                                                                                     ##STR52##  H          O H     OMe  OMe    CH                     II-603                                                                            Me                                                                                     ##STR53##  H          O H     Me   OMe    CH                     II-604                                                                            Me                                                                                     ##STR54##  H          O H     Me   OMe    N                      II-605                                                                            Me                                                                                     ##STR55##  H          O H     OMe  OMe    CH                     II-606                                                                            Me                                                                                     ##STR56##  H          O H     Me   OMe    CH                     II-607                                                                            Me                                                                                     ##STR57##  H          O H     Me   OMe    N                      II-608                                                                            Me                                                                                     ##STR58##  H          O H     OMe  OMe    CH                     II-609                                                                            Me                                                                                     ##STR59##  H          O H     Me   OMe    CH                     II-610                                                                            Me                                                                                     ##STR60##  H          O H     Me   OMe    CH                     II-611                                                                            Me      OC.sub.2 H.sub.4 O*    O H     OMe  OMe    CH                     II-612                                                                            Me      OC.sub.2 H.sub.4 O*    O H     Me   OMe    CH                     II-613                                                                            Me      OC.sub.2 H.sub.4 O*    O H     Me   OMe    N                      II-614                                                                            Me      SC.sub.2 H.sub.4 S*    O H     OMe  OMe    CH                     II-615                                                                            Me      SC.sub.2 H.sub.4 S*    O H     Me   OMe    CH                     II-616                                                                            Me      SC.sub.2 H.sub.4 S*    O H     Me   OMe    N                      II-617                                                                            Me      OCH.sub.2 O*           O H     OMe  OMe    CH                     II-618                                                                             ##STR61##                                                                            Cl          H          O H     OMe  OMe    CH                     II-619                                                                             ##STR62##                                                                            Cl          H          O H     OMe  OMe    CH                     II-620                                                                             ##STR63##                                                                            Cl          H          O H     OMe  OMe    CH                     II-621                                                                            COMe    Cl          H          O H     OMe  OMe    CH                     II-622                                                                            COEt    Cl          H          O H     OMe  OMe    CH                     II-623                                                                            COPr    Cl          H          O H     OMe  OMe    CH                     II-624                                                                            COPr-i  Cl          H          O H     OMe  OMe    CH                     II-625                                                                            COPh    Cl          H          O H     OMe  OMe    CH                     II-626                                                                            SO.sub.2 Me                                                                           Cl          H          O H     OMe  OMe    CH                     II-627                                                                            SO.sub.2 Et                                                                           Cl          H          O H     OMe  OMe    CH                     II-628                                                                            SO.sub.2 Ph                                                                           Cl          H          O H     OMe  OMe    CH                     II-629                                                                            COOMe   Cl          H          O H     OMe  OMe    CH                     II-630                                                                            COOEt   Cl          H          O H     OMe  OMe    CH                     II-631                                                                            COOPh   Cl          H          O H     OMe  OMe    CH                     II-632                                                                            CONMe.sub.2                                                                           Cl          H          O H     OMe  OMe    CH                     II-633                                                                            SO.sub.2 NMe.sub.2                                                                    Cl          H          O H     OMe  OMe    CH                     II-634                                                                            Ph      Cl          H          O H     Me   OMe    N                      II-635                                                                            CH.sub.2 OMe                                                                          Cl          H          O H     OMe  OMe    CH                     II-636                                                                            CH.sub.2 OBn                                                                          Cl          H          O H     OMe  OMe    CH                     II-637                                                                            CH.sub.2 CH.sub.2 F                                                                   Cl          H          O H     OMe  OMe    CH                     II-638                                                                            CH.sub.2 CH.sub.2 Cl                                                                  Cl          H          O H     OMe  OMe    CH                     II-639                                                                            CF.sub.3                                                                              Cl          H          O H     OMe  OMe    CH                     II-640                                                                            CH.sub.2 F                                                                            Cl          H          O H     OMe  OMe    CH                     II-641                                                                            CH.sub.2 CHCH.sub.2                                                                   OMe         H          O H     OMe  OMe    CH                     II-642                                                                            COCF.sub.3                                                                            Cl          H          O H     OMe  OMe    CH                     II-643                                                                             ##STR64##                                                                            Cl          H          O H     OMe  OMe    CH                     II-644                                                                            Me      Cl          H          O CH.sub.3 OCH.sub.2                                                                  OMe  OMe    CH                     II-645                                                                            Me      Cl          H          O H     OMe  NMe.sub.2                                                                            N                      II-646                                                                            Me      Cl          H          O H     OMe  NHMe   N                      II-648                                                                            Me      ONCHMe      H          O H     OMe  OMe    CH                     II-649                                                                            Me      ONCMe.sub.2 H          O H     OMe  OMe    CH                     II-650                                                                            Me      ONCHBn      H          O H     OMe  OMe    CH                     II-651                                                                            Me      OCH.sub.2 CH.sub.2 F                                                                      H          O H     OMe  Me     CH 167-170             II-652                                                                            Me      OCH.sub.2 CH.sub.2 F                                                                      H          O H     OMe  Me     N  167-169             II-653                                                                            Me      F           H          O H     NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N  108-112             II-654                                                                            Me      SO.sub.2 NMe.sub.2                                                                        H          O H     OMe  Me     N  191-193             II-655                                                                            Me      CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                             H          O H     OMe  OMe    CH                     II-656                                                                            Me      CO.sub.2 CH.sub. 2 CF.sub.3                                                               H          O H     OMe  OMe    CH                     II-657                                                                            Me      CO.sub.2 CH.sub.2 OMe                                                                     H          O H     OMe  OMe    CH                     II-658                                                                            Me      CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                             H          O H     OMe  OMe    CH                     II-659                                                                            Me      CO.sub.2 CH.sub.2 CF.sub.3                                                                H          O H     OMe  OMe    CH                     II-660                                                                            Me      CO.sub.2 CH.sub.2 OMe                                                                     H          O H     OMe  OMe    CH                     __________________________________________________________________________     *R.sup.3 represents the 5position.                                       

The following processes may, for example, be mentioned as the processesfor producing the compounds of the present invention. However, theprocesses are not limited to such specific processes.

Common processes for producing the compound [I] or [II] of the presentinvention are shown by the following Processes 1 to 3. ##STR65##(wherein R¹, R², R³, A, B, Z, X and Y have the same meanings as definedabove.)

Namely, the compound of the present invention represented by the formula[I] or [II] can be produced by reacting an intermediate for itsproduction of the present invention represented by the formula [I-a] or[II-a] (hereinafter referred to as an intermediate, and the process forits production will be described hereinafter) and a compound representedby the formula [III].

This reaction is usually conducted in a solvent or without solvent, ifnecessary, in the presence of a base. The range of the reactiontemperature is a range from -20° C. to the boiling point of the solvent,and the range of the reaction time is a range of from 0.5 hour to 24hours. With respect to the amounts of the compounds to be subjected tothe reaction, the amounts of the compound represented by the formula[III] and the base are respectively independently from 1 to 1.5equivalent relative to one equivalent of the intermediate represented bythe formula [I-a] or [II-a].

As the solvent, an aromatic hydrocarbon such as benzene, xylene ortoluene, a halogenated hydrocarbon such as chloroform, carbontetrachloride, dichloroethane, chlorobenzene or dichlorobenzene, anether such as diethyl ether, dioxane, tetrahydrofuran (THF), isopropylether (IPE) or diethylene glycol dimethyl ether, an alcohol such asmethanol, ethanol or 2-propanol, an ester such as ethyl acetate or butylacetate, a nitro compound such as nitromethane or nitrobenzene, anitrile such as acetonitrile or isobutyronitrile, or an aprotic polarsolvent such as formamide, N,N-dimethylformamide (DMF),N,N-dimethylacetamide (DMAC), dimethylsulfoxide (DMSO) orN-methylpyrrolidone (NMP), may, for example, be mentioned.

As the base, an organic base such as pyridine, triethylamine,1,4-diazabicyclo[2.2.2] octane, 1,8-diazabicyclo[5.4.0]-7-undecene(DBU), N,N-diethylaniline or diethyl-methylamine, an inorganic base suchas sodium hydroxide, potassium hydroxide, sodium carbonate, potassiumcarbonate or sodium hydride, or an alkali metal alkoxide such as sodiummethoxide or sodium ethoxide, may, for example, be mentioned.

Further, the compound represented by the formula [III] can be producedby reacting a compound represented by the formula [IV] in Process 2 withphenyl chloroformate, phenyl chlorothio-O-formate or phenylchlorodithioformate, in a proper solvent in the presence of a base.##STR66## (wherein R¹, R², R³, A, B, X, Y and Z have the same meaningsas defined above.)

The compound of the present invention represented by the formula [I] or[II] can be produced by reacting a compound represented by the formula[I-b] or [II-b] and a compound represented by the formula [IV]. Thecompound represented by the formula [I-b] or [II-b] can be produced byreacting an intermediate represented by the formula [I-a] or [II-a] withphosgene or thiophosgene in a suitable solvent.

This reaction is usually conducted in a solvent or without solvent, ifnecessary, in the presence of a base. The range of the reactiontemperature, the range of the reaction time, and the solvent and thebase to be used in the reaction are the same as in Process 1. Withrespect to the amounts of the compounds to be subjected to the reaction,the amounts of the compounds represented by the formula [IV] and thebase are respectively independently from 1 to 1.5 equivalent relative toone equivalent of the compound represented by the formula [I-b] or[II-b]. ##STR67## (wherein R¹, R², R³, A, B, X, Y and Z have the samemeanings as defined above.)

The compound of the present invention represented by the formula [I] or[II] can be produced by reacting a compound represented by the formula[I-c] or [II-c] and a compound of the formula [IV]. The compoundrepresented by the formula [I-c] or [II-c] can be produced by reactingan intermediate represented by the formula [I-a] or [II-a] with phenylchloroformate, phenyl chlorothio-O-formate or phenylchlorodithioformate, in a suitable solvent in the presence of a base. Itmay also be produced by reacting a compound represented by the formula[I-b] or [II-b] with phenol or thiophenol.

This reaction is usually conducted in a solvent or without solvent, ifnecessary, in the presence of a base. The range of the reactiontemperature, the range of the reaction time, and the solvent and thebase to be used in the reaction are the same as in Process 1. Withrespect to the amounts of the compounds to be subjected to the reaction,the amounts of the compound represented by the formula [IV] and the baseare respectively independently from 1 to 1.5 equivalent relative to oneequivalent of the compound represented by the formula [I-c] or [II-c]. Aprocess for producing an intermediate of the formula [I-a] useful forthe production of the compound of the present invention will be shown byProcess 1 For Producing An Intermediate, and a process for producing anintermediate of the formula [II-a] will be shown by Process 2 ForProducing An Intermediate. However, the processes are not limited tosuch specific examples.

Process 1 For Producing An Intermediate

Production of the formula [I-a] ##STR68## (wherein R¹ represents ahydrogen atom, an alkyl group, a benzyl group or a phenyl group, R² andR³ represent a hydrogen atom, an alkyl group, a halogen atom, a nitrogroup, an alkoxy group, a haloalkoxy group or a haloalkyl group, and Lrepresents a halogen atom.)

Namely, a compound represented by the formula [V] is reacted with thecorresponding hydrazine derivative, for example, in DMSO, to obtain acompound represented by the formula [VI]. Further, in concentratedhydrochloric acid, a diazonium salt is formed, and this is reacted withsulfurous acid gas in a solvent such as acetic acid in the presence ofcopper chloride to obtain a compound represented by the formula [VII].This is reacted with excess t-butylamine to produce a compoundrepresented by the formula [I-d]. Then, the t-butyl group is removedwith excess trifluoroacetic acid to obtain an intermediate representedby the formula [I-a].

Process 2 For Producing An Intermediate

Production of the formula [II-a] ##STR69## (wherein R¹ represents analkyl group, a haloalkyl group, a benzyl group or a phenyl group, and R²and R³ represent a hydrogen atom, an alkyl group, a halogen atom, analkoxy group, a phenyl group, a benzyl group or a haloalkoxy group.)

Namely, a compound represented by the formula [IX] can be produced byreacting a compound represented by the formula [VIII] with n-butyllithium, for example, in ethyl ether, within a temperature range of from-40° to -20° C., followed by blowing in sulfurous acid gas. Anintermediate represented by the formula [II-a] can be produced by addingan aqueous solution of the compound represented by the formula [IX] toan aqueous solution of a mixture of hydroxylamine-O-sulfonic acid and abase under cooling with ice.

In this reaction formula, the compound of the formula [VIII] can beproduced by a method disclosed in a known literature such as [LiebigsAnn. Chem., 908 (1980)], [Org. Synth. Coll. Vol. V, 650], [J. Chem. Soc.Perkin Trans. II, 1695, (1975)], or [Org. Synth, Coll. Vol. V, 941].

The intermediate represented by the formula [I-a] or [II-a] can beproduced also by the following process.

Process 3 For Producing An Intermediate

Production of the formula [I-a] or [II-a] ##STR70## (wherein R¹represents an alkyl group, a cycloalkyl group, a haloalkyl group, analkoxyalkyl group, a benzyloxyalkyl group, a benzyl group, adialkylaminocarbonyl group, an alkoxycarbonyl group, a alkylsulfonylgroup, a phenylsulfonyl group, a dialkylaminosulfonyl group, ahaloalkylcarbonyl group, an alkylcarbonyl group, a benzoyl group or analkenyl group, R² or R³ represents a hydrogen atom, a halogen atom, analkoxy group, a haloalkoxy group, a haloalkyl group, an alkoxycarbonylgroup, a phenyl group or a benzyl group, L represents a halogen atom,and M represents a bromine atom or a chlorine atom.)

Namely, a compound represented by the formula [X] is reacted withN-bromosuccinimide, N-chlorosuccinimide, or bromine or chlorine incarbon tetrachloride in the presence of a light and a radical reactioninitiating agent to obtain a compound represented by the formula [XI].The compound represented by the formula [XI] is reacted with thiourea toobtain a compound represented by the formula [XII]. The compoundrepresented by the formula [XII] is reacted with chlorine or bromine ina mixed solution of acetic acid and water to obtain a compoundrepresented by the formula [XIII]. Then, this compound is reacted witht-butylamine to obtain a compound represented by the formula [XIV]. Thecompound represented by the formula [XIV] is reduced to obtain acompound represented by the formula [XV]. The compound represented bythe formula [XV] and isoamylnitrous acid are reacted, followed byreaction with hydrochloric acid to obtain a compound represented by theformula [XVI]. The compound represented by the formula [XVI] is reactedwith e.g. an alkyl halide or a benzyl halide to obtain a compoundrepresented by the formula [I-d] or [II-d].

The compound represented by the formula [XVI], [I-d] or [II-d] can beconverted to a compound represented by the formula [XVII] and anintermediate represented by the formula [I-a] or [II-a], respectively,by removing the t-butyl group with trifluoroacetic acid, as shown inProcess 1 For Producing An Intermediate.

Further, the compound represented by the formula [XVII] is reacted withR¹ L (wherein R¹ and L have the same meanings as defined above) toobtain intermediates of the formulas [I-a] and [II-a].

The intermediate represented by the formula [I-a] may be prepared byvarious processes depending upon the types of the substituents. However,it can be produced by the processes represented by the following Process4 For Producing An Intermediate and Processes 5-1 to 5-3 For ProducingAn Intermediate.

Process 4 For Producing An Intermediate ##STR71## (wherein R¹ representsa-hydrogen atom, an alkyl group, a benzyl group or a phenyl group, R²represents a halogen atom, preferably a fluorine atom, R³ has the samemeaning as defined above, and R⁴ represents an alkoxy group, analkoxyalkoxy group, a benzyloxy group, a cycloalkylalkoxy group, ahaloalkoxy group, a dialkylaminoalkoxy group, an alkylthio group, analkylamino group, a dialkylamino group or a benzylamino group.)

Namely, in this reaction, an intermediate represented by the formula[I-a ] or [II-a ] is reacted with a compound represented by the formulaR⁴ --H (wherein R⁴ has the same meaning as defined above) in a polarsolvent such as DMSO, DMF, DMAC or NMP in the presence of a base such assodium hydride, potassium hydride, potassium carbonate, potassiumt-butoxide, sodium hydroxide or potassium hydroxide, to obtain anintermediate represented by the formula [I-e] or [II-e], respectively.

Process 5-1 For Producing An Intermediate ##STR72## (wherein R¹represents an alkyl group, a benzyl group or a phenyl group, R³ has thesame meaning as defined above, R⁵ represents an alkyl group, a benzylgroup, an alkenyl group, an alkynyl group, a haloalkenyl group, ahaloalkyl group, an alkoxyalkyl group, an alkoxycarbonylalkyl group or acyanoalkyl group, and L¹ represents a halogen atom, an alkylsulfonyloxygroup, a haloalkylsulfonyloxy group or a benzenesulfonyloxy group whichmay be substituted.) Namely, in this reaction formula, an intermediaterepresented by the formula [I-f] or [II-f] is reacted with a compoundrepresented by the formula R⁵ --L¹ (wherein R⁵ and L¹ have the samemeanings as defined above) in a suitable solvent in the presence of abase, to obtain an intermediate represented by the formula [I-g] or[II-g], respectively.

The intermediate represented by the formula [I-f] or [II-f] can beproduced by the following process. ##STR73## (wherein R¹ represents analkyl group, a benzyl group or a phenyl group, R² represents a halogenatom, preferably a fluorine atom, R³ represents a hydrogen atom, ahalogen atom, an alkyl group, a haloalkyl group, a haloalkoxy group oran alkoxy group, and R⁸ represents an alkyl group, a benzyl group or acycloalkyl group, preferably a cyclopropylmethyl group.)

Namely, in this reaction formula, an intermediate represented by theformula [I-a] or [II-a] is reacted with a compound of the formula R⁸--OH (wherein R⁸ has the same meaning as defined above) in a suitablesolvent in the presence of a base, to obtain an intermediate representedby the formula [I-h] or [II-h], which is further subjected to removal ofthe protecting group to obtain an intermediate of the formula [I-f] or[II-f], respectively.

Process 5-2 For Producing An Intermediate ##STR74## (wherein R¹represents an alkyl group, a benzyl group or a phenyl group, and R³ andR⁵ have the same meanings as defined above.)

Namely, in this reaction formula, an intermediate represented by theformula [I-f] or [II-f] is subjected to a Mitsunobu reaction (asdisclosed in Organic Reactions Vol. 42, p-335) using a compoundrepresented by the formula R⁵ --OH (wherein R⁵ has the same meaning asdefined above) in a suitable solvent, to obtain an intermediate of theformula [I-g] or [II-g], respectively.

Process 5-3 For Producinq An Intermediate ##STR75## (wherein R¹represents an alkyl group, a benzyl group or a phenyl group, R³, R⁵ andL¹ have the same meanings as defined above, and R⁶ represents an alkylgroup, preferably a methyl group.)

Namely, in this reaction formula, an intermediate represented by theformula [I-f] or [II-f] is reacted with acetal of DMF to obtain acompound represented by the formula [I-i] or [II-i], which is thenreacted with a compound represented by the formula R⁵ --L¹ (wherein R⁵and L¹ have the same meanings as defined above) in a suitable solvent inthe presence of a base to obtain a compound represented by the formula[I-j] or [II-j], which is then hydrolyzed with an acid or alkali toobtain an intermediate represented by the formula [I-g] or [II-g].

Now, specific compounds of the intermediate represented by the formula[I-a] or [II-a] will be listed in Table 3.

                  TABLE 3                                                         ______________________________________                                        Inter-                                                                        mediate                                                                       No.    R.sup.1                                                                              R.sup.2         R.sup.3 mp. (°C.)                        ______________________________________                                         ##STR76##                                                                    1      Me     Ph              H                                               2      Me     Bn              H                                               3      Me     SH              H                                               4      Me     SMe             H                                               5      Me     SEt             H       223-225                                 6      Me     SPr             H       208-209                                 7      Me     SO.sub.2 Me     H                                               8      Me     SO.sub.2 Et     H       271-273                                 9      Me     SOMe            H                                               10     Me     SO.sub.2 NHMe   H                                               11     Me     SO.sub.2 NHOMe  H                                               12     Me     SO.sub.2 NMe.sub.2                                                                            H       248-252                                 13     Me     SO.sub.2 NHBn   H                                               14     Me     SO.sub.2 NHPh   H                                               15     Me     SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                                H                                               16     Me     SO.sub.2 NHCH.sub.2 CCH                                                                       H                                               17     H      Cl              H       215-217                                 18     Me     Cl              H       268-270                                 19     Me     Cl              5-Cl    283-285                                 20     Et     Cl              H       180-182                                 21     Ph     Cl              H                                               22     Bn     Cl              H                                               23     Me     H               H       178-180                                 24     Me     F               if      221-223                                 25     Me     Br              H       285-287                                 26     Me     Me              H                                               27     Me     CN              H       274-281                                 28     Me     CF.sub.3        H                                               29     Me     H               5-Cl                                            30     Me     H               6-Cl                                            31     Me     H               7-Cl                                            32     Me     COH             H                                               33     Me     COMe            H                                               34     Me     COEt            H                                               35     Me     COPh            H                                               36     Me     CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H                                               37     Me     CO.sub.2 CH.sub.2 CCH                                                                         H                                               38     Me     COBn            H                                               39     Me     NO.sub.2        H       249-251                                 40     Me     NH.sub.2        H                                               41     Me     NHMe            H                                               42     Me     NMe.sub.2       H                                               43     Me     NHCOMe          H                                               44     Me     NHCOPh          H                                               45     Me     NHCOCH.sub.2 Cl H                                               46     Me     NHSO.sub.2 CH.sub.3                                                                           H                                               47     Me     NHSO.sub.2 Ph   H                                               48     Me     CO.sub.2 H      H                                               49     Me     CO.sub.2 Me     H       233-234                                 50     Me     CO.sub.2 Et     H       193-195                                 51     Me     CO.sub.2 Pr     H       185-188                                 52     Me     CO.sub.2 Pr-i   H       219-220                                 53     Me     CO.sub.2 Bu     H       167-168                                 54     Me     CO.sub.2 Pen    H                                               55     Me     CO.sub.2 Bn     H                                               56     Me     CO.sub.2 Ph     H                                               57     Me     CO.sub.2 CH.sub.2 CH.sub.2 F                                                                  H                                               58     Me     CO.sub.2 Me     5-F                                             59     Et     CO.sub.2 Me     H                                               60     Bu     CO.sub.2 Me     H                                               61     Bn     CO.sub.2 Me     H                                               62     Ph     CO.sub.2 Me     H                                               63     H      CO.sub.2 Et     H                                               64     Me     OH              H                                               65     Me     OMe             H       268-270                                 66     Me     OEt             H       230-233                                 67     Me     OPr             H       210-212                                 68     Me     OPr-i           H       200-201                                 69     Me     OBu             H       203-205                                 70     Me     OBn             H                                               71     Me     OBn(4-Cl)       H                                               72     Me     OBn(3-OMe)      H                                               73     Me     OBn(2-Me)       H                                               74     Me     OPh             H                                               75     Me     OPh(4-Cl)       H                                               76     Me     OPh(3-OMe)      H                                               77     Me     OPh(2-Me)       H                                               78     Me     OCH.sub.2 CHCH.sub.2                                                                          H                                               79     Me     OCH.sub.2 CCH   H                                               80     Me     OCH.sub.2 CF.sub.3                                                                            H                                               81     Me     OCH.sub.2 CH.sub.2 OMe                                                                        H                                               82     Me     OCH.sub.2 CH.sub.2 OPh                                                                        H                                               83     Me     OCOMe           H                                               84     Me     CONH.sub.2      H                                               85     Me     CONHMe          H                                               86     Me     CONHEt          H                                               87     Me     CONHPr          H                                               88     Me     CONMe.sub.2     H       274-275                                 89     Me     CONEt.sub.2     H                                               90     Me     CONHBn          H                                               91     Me     CONHPh          H                                               92     Me     CONHCH.sub.2 CHCH.sub.2                                                                       H                                               93     Me     CONHCH.sub.2 CCH                                                                              H                                               94     Me     CONHOMe         H                                               95     Me     H               5-F                                             96     Me     SO.sub.2 NH.sub.2                                                                             H                                               97     Me     SPr-i           H       228-231                                 98     Me     OCH.sub.2 CH.sub.2 OEt                                                                        H                                               99     Me     OCH.sub.2 CH.sub.2 OPr-i                                                                      H                                               100    Me     OCH.sub.2 CH.sub.2 OBu                                                                        H                                               101    Me     OCH.sub.2 CH.sub.2 OBu-t                                                                      H                                               102    Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                                  H                                               103    Me     OCH.sub.2 COOEt H                                               104    Me     OCH.sub.2 CH.sub.2 Cl                                                                         H                                               105    Me     OCH.sub.2 CH.sub.2 F                                                                          H                                               106    Me     OCH.sub.2 OCH.sub.3                                                                           H                                               107    Me     OCH(CF.sub.3)Me H                                               108    Me     H               5-OMe                                           109    Me     H               5-OEt                                           110    Me     H               5-OPr                                           111    Et     CO.sub.2 Me     H                                               112    Et     Br              H                                               113    Me     OCHF.sub.2      H                                               114    Me     SO.sub.2 Pr     H       270-272                                 115    Me     SO.sub.2 Pr-i   H       260-263                                 116    Me     SO.sub.2 Bu     H       287-290                                 117    Me     SBu             H       187-189                                 118    Me     OMe             5-Cl                                            119    Me     NHBn            H                                               120    Me     OCH.sub.2 Bu-t  H                                               121    Me     OCH.sub.2 CHF.sub.2                                                                           H                                               122    H      NO.sub.2        H       >300                                    123    H      Br              H       183-186                                 124    H      COOCH.sub.3     H       243-247                                 125    Me     H               5-CO.sub.2 Me                                                                         238-241                                  ##STR77##                                                                    126    Me     Ph              H                                               127    Me     Bn              H                                               128    Me     SH              H                                               129    Me     SMe             H                                               130    Me     SEt             H       145-147                                 131    Me     SPr             H                                               132    Me     SO 2Me          H                                               133    Me     SO 2Et          H       167-169                                 134    Me     SOMe            H                                               135    Me     SO.sub.2 NHMe   H                                               136    Me     SO.sub.2 NHOMe  H                                               137    Me     SO.sub.2 NMe.sub.2                                                                            H       218-220                                 138    Me     SO.sub.2 NHBn   H                                               139    Me     SO.sub.2 NHPh   H                                               140    Me     SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                                H                                               141    Me     SO.sub.2 NHCH.sub.2 C CH                                                                      H                                               142    H      Cl              H       215-217                                 143    Me     Cl              H       173-175                                 144    Me     Cl              5-Cl                                            145    Et     Cl              H       182-184                                 146    Ph     Cl              H       220-221                                 147    Bn     Cl              H                                               148    Me     H               H       181-183                                 149    Me     F               H       151-152                                 150    Me     Br              H       182-183                                 151    Me     Me              H       149-151                                 152    Me     CN              H       227-228                                 153    Me     CF.sub.3        H                                               154    Me     H               5-Cl    186-188                                 155    Me     H               6-Cl    206-207                                 156    Me     H               7-Cl    175-177                                 157    Me     COH             H                                               158    Me     COMe            H                                               159    Me     COEt            H                                               160    Me     COPh            H                                               161    Me     CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H                                               162    Me     CO.sub.2CH.sub.2 CCH                                                                          H                                               163    Me     COBn            H                                               164    Me     NO.sub.2        H       193-194                                 165    Me     NH.sub.2        H                                               166    Me     NHMe            H       179-181                                 167    Me     NMe.sub.2       H       197-200                                 168    Me     NHCOMe          H                                               169    Me     NHCOPh          H                                               170    Me     NHCOCH.sub.2 Cl H                                               171    Me     NHSO.sub.2 CH.sub.3                                                                           H                                               172    Me     NHSO.sub.2 Ph   H                                               173    Me     CO.sub.2 H      H                                               174    Me     CO.sub.2 Me     H       160-163                                 175    Me     CO.sub.2 Et     H       135-137                                 176    Me     CO.sub.2 Pr     H       130-132                                 177    Me     CO.sub.2 Pr-i   H       145-147                                 178    Me     CO.sub.2 Bu     H       113-114                                 179    Me     CO.sub.2 Pen    H                                               180    Me     CO.sub.2 Bn     H                                               181    Me     CO.sub.2 Ph     H                                               182    Me     CO.sub.2 CH.sub.2 CH.sub.2 F                                                                  H                                               183    Me     CO.sub.2 Me     5-F                                             184    Et     CO.sub.2 Me     H                                               185    Bu     CO.sub.2 Me     H                                               186    Bn     CO.sub.2 Me     H                                               187    Ph     CO.sub.2 Me     H                                               188    H      CO.sub.2 Et     H                                               189    Me     OH              H       180-181                                 190    Me     OMe             H       265-268                                 191    Me     OEt             H       184-185                                 192    Me     OPr             H       186-188                                 193    Me     OPr-i           H       205-206                                 194    Me     OBu             H       152-154                                 195    Me     OBn             H                                               196    Me     OBn(4-Cl)       H                                               197    Me     OBn(3-OMe)      H                                               198    Me     OBn(2-Me)       H                                               199    Me     OPh             H                                               200    Me     OPh(4-Cl)       H                                               201    Me     OPh(3-OMe)      H                                               202    Me     OPh(2-Me)       H                                               203    Me     OCH.sub.2 CHCH.sub.2                                                                          H       143-144                                 204    Me     OCH.sub.2 CCH   H       180-181                                 205    Me     OCH.sub.2 CF.sub.3                                                                            H       182-183                                 206    Me     OCH.sub.2 CH.sub.2 OMe                                                                        H       174-176                                 207    Me     OCH.sub.2 CH.sub.2 OPh                                                                        H                                               208    Me     OCOMe           H                                               209    Me     CONH.sub.2      H                                               210    Me     CONHMe          H                                               211    Me     CONHEt          H                                               212    Me     CONHPr          H                                               213    Me     CONMe.sub.2     H       267-270                                 214    Me     CONEt.sub.2     H                                               215    Me     CONHBn          H                                               216    Me     CONHPh          H                                               217    Me     CONHCH.sub.2 CHCH.sub.2                                                                       H                                               218    Me     CONHCH.sub.2 CCH                                                                              H                                               219    Me     CONHOMe         H                                               220    Me     H               5-F     174-175                                 221    Me     SO.sub.2 NH.sub.2                                                                             H                                               222    Me     SPr-i           H       134-135                                 223    Me     OCH.sub.2 CH.sub.2 OEt                                                                        H       116-120                                 224    Me     OCH.sub.2 CH.sub.2 OPr-i                                                                      H       118-119                                 225    Me     OCH.sub.2 CH.sub.2 OBu                                                                        H       144-145                                 226    Me     OCH.sub.2 CH.sub.2 OBu-t                                                                      H       183-184                                 227    Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                                  H       184-187                                 228    Me     OCH.sub.2 COOEt H       116-120                                 229    Me     OCH.sub.2 CH.sub.2 Cl                                                                         H       177-179                                 230    Me     OCH.sub.2 CH.sub.2 F                                                                          H       178-180                                 231    Me     OCH.sub.2 OCH.sub.3                                                                           H       163- 165                                232    Me     OCH(CF.sub.3)Me H       165-167                                 233    Me     H               5-OMe   169-172                                 234    Me     H               5-OEt   152-153                                 235    Me     H               5-OPr   149-151                                 236    Et     CO.sub.2 Me     H       123-125                                 237    Et     Br              H                                               238    Me     OCHF.sub.2      H       164-166                                 239    Me     SO.sub.2 Pr     H       176-178                                 240    Me     SO.sub.2 Pr-i   H       220-221                                 241    Me     SO.sub.2 Bu     H       156-158                                 242    Me     SBu             H       162-164                                 243    Me     OMe             5-Cl    161-163                                 244    Me     NHBn            H       189-191                                 245    Me     OCH.sub.2 Bu-t  H       207-208                                 246    Me     OCH.sub.2 CHF.sub.2                                                                           H       186-188                                 247    Me     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                                 H       139-140                                 248    Me     OMe             H       138-140                                 249    Me     Cl              H       176-178                                 250    Me     OCH.sub.2 OEt   H       148-150                                 251    Me     OCH.sub.2 C(CH.sub.3 )CH.sub.2                                                                H       132-134                                 252    Me     OCH.sub.2 CHC(Me).sub.2                                                                       H       141-143                                 253    Me     OCH.sub.2 CHCHCl                                                                              H       164-166                                 254    Me                                                                                    ##STR78##      H       139-141                                 255    Me     OCH.sub.2 OBn   H       156-158                                 ______________________________________                                    

BEST MODE FOR CARRYING OUT THE INVENTION

Now, the present invention will be specifically explained by describingthe process for producing the intermediate and the process for producingthe compound of the present invention as Preparation Examples.

PREPARATION EXAMPLE 1 Preparation of1-methyl-4-fluoro-1H-indazole-3-sulfonamide (Intermediate No. 24)

75 g (539 mmol) of 2,6-difluorobenzonitrile was added to 300 ml of DMSO,and 33 g (716 mmol) of methylhydrazine was dropwise added thereto withstirring. The reaction proceeded exothermically, and the dropwiseaddition was continued while maintaining the temperature at a level offrom 80° to 100° C. After returning to room temperature, the mixture waspoured into a large excess amount of cool water, whereupon crystals werecollected by filtration and dried in air to obtain 72 g (yield: 81%) of3-amino-1-methyl-4-fluoro-1H-indazole (compound represented by theformula [VI] (slightly yellow crystals).

Then, 70 g (424 mmol) of 3-amino-1-methyl-4-fluoro-1H-indazole wasdissolved in 200 ml of acetic acid, and 140 ml of concentratedhydrochloric acid was added thereto. The mixture was vigorously stirred,and a solution having 33 g (478 mmol) of sodium nitrite dissolved in 60ml of water, was gradually dropwise added thereto within a range of from-5° to -10° C. The diazonium salt solution thus obtained, was graduallydropwise added to a mixture having 17 g (100 mmol) of cupric chloridedihydrate added to a solution obtained by blowing sulfurous acid gasinto 370 ml of acetic acid until saturation (120 g). After completion ofthe dropwise addition, stirring was continued for one hour at atemperature of not higher than 0° C., and then the mixture was pouredinto a large excess amount of cold water, whereupon crystals werecollected by filtration and dried in air to obtain 70 g (yield: 66%) of1-methyl-4-fluoro-1H-indazole-3-sulfonylchloride (compound representedby the formula [VII]) (slightly purple crystals).

Further, 13.9 g (56 mmol) of1-methyl-4-fluoro-1H-indazole-3-sulfonylchloride in 50 ml of THF, wasadded to 12.9 g (177 mmol) of t-butylamine in 100 ml of THF, and themixture was stirred at room temperature overnight. After completion ofthe reaction, the mixture was poured into a large excess amount ofwater, whereupon the crystals were collected by filtration and dried inair to obtain 15.9 g (yield: 99.6%) of3-(N-t-butylsulfamoyl)-1-methyl-4-fluoro-1H-indazole (compoundrepresented by the formula [I-d]) (slightly purple crystals).

15 g (53 mmol) of 3-(N-t-butylsulfamoyl)-1-methyl-4-fluoro-1H-indazolewas added to 50 ml of trifluoroacetic acid, and the mixture was stirredovernight. After completion of the reaction, trifluoroacetic acid wasdistilled off under reduced pressure, and the residue was washed withn-hexane to obtain 10.5 g (yield: 86.8%) of1-methyl-4-fluoro-1H-indazole-3-sulfonamide (slightly purple crystals).Melting point: 221°-223° C.

PREPARATION EXAMPLE 2 Preparation of1-(1-methyl-4-fluoro-1H-indazole-3-sulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea(Compound No. I-26)

0.35 g (2.3 mmol) of DBU was added to a solution containing 0.5 g (2.3mmol) of 1-methyl-4-fluoro-1H-indazole-3-sulfonamide obtained inPreparation Example 1 and 0.62 g (2.3 mmol) of phenyl(4,6-dimethoxypyrimidin-2-yl)carbamate in 20 ml of acetonitrile, and themixture was stirred at room temperature for 12 hours. The mixture waspoured into ice water and acidified with citric acid, whereupon theformed crystals were collected by filtration and washed with ice water,IPE and ethyl ether to obtain 0.49 g (yield: 52%) of the desired product(colorless needle like crystals). Melting point: 205°-209° C.

PREPARATION EXAMPLE 3-1 Preparation of methyl2-bromomethyl-3-nitrobenzoate (compound represented by the formula [XI])

A suspension containing 98 g (0.5 mol) of methyl2-methyl-3-nitrobenzoate, 100 g (0.56 mol) of N-bromosuccinimide and 1 gof benzoyl peroxide in carbon tetrachloride (800 ml), was refluxed for 3days under irradiation with 500 W. The suspension was cooled to roomtemperature and subjected to filtration, whereupon the filtrate wasconcentrated. To the residue, ethyl ether (200 ml) and IPE (200 ml) wereadded, whereupon the formed crystals were collected by filtration toobtain 121 g (yield: 88.3%) of the desired product. Melting point:65°-67° C.

PREPARATION EXAMPLE 3-2 Preparation ofS-(2-methoxycarbonyl-6-nitrobenzyl)-thiouronium bromide (compoundrepresented by the formula [III]

In methanol (2 l), 207 g (0.76 mol) of the product from PreparationExample 3-1 and 57.6 g (0.76 mol) of thiourea were refluxed for 12hours. After cooling, methanol was distilled off, and ethyl acetate (1l) was added to the residue. The product was subjected to filtration.This product was used for the subsequent reaction without purification.The obtained amount: 246 g (yield: 93%)

PREPARATION EXAMPLE 3-3 Preparation of methyl2-(t-butylaminosulfonylmethyl)-3nitrobenzoate (compounds represented bythe formulas [XIII] and [XIV])

110 g (0.32 mol) of the product from Preparation Example 3-2 in water (2l) and acetic acid (1 l), was cooled to 5° C. and chlorine was blownthereto for 4 hours at a temperature of from 5° to 10° C. And, themixture was stirred at room temperature for one hour. Then, the productwas collected by filtration and washed with ice water and then dissolvedin 1 l of dichloromethane. To this solution, 54 g (0.74 mol) oft-butylamine was dropwise added at a temperature of from 0° to 5° C.Then, the mixture was stirred at room temperature for 2 hours. Theorganic layer was washed with water and then concentrated. IPE was addedto the residue, followed by filtration to obtain 63 g (yield: 60.1%) ofthe desired product. This product was used for the subsequent reactionwithout purification.

PREPARATION EXAMPLE 3-4 Preparation of methyl3-amino-2-(t-butylaminosulfonylmethyl)benzoate (compound represented bythe formula [XV])

A solution containing 48 g (0.145 mol) of the product from PreparationExample 3-3 and 164 g (0.73 mol) of stannous chloride dihydrate in 300ml of ethanol, was refluxed for 2 hours. After cooling, it was added to2 l of ethyl acetate, and powdery sodium hydrogencarbonate (500 g) wasgradually added thereto. The formed salt was collected by filtration andthoroughly washed with ethyl acetate. The organic layer was concentratedto obtain 35.9 g (yield: 82.4%) of the desired product. Melting point:123°-125° C.

PREPARATION EXAMPLE 3-5 Preparation of methyl3-(t-butylaminosulfonyl)-1H-indazole-4-carboxylate (compound representedby the formula [XVI])

A suspension containing 30 g (0.1 mol) from Preparation Example 3-4,30.6 g (0.3 mol) of acetic anhydride and 10 g (0.102 mol) of potassiumacetate in benzene (500 ml), was heated to 80° C., and at the sametemperature, 17.6 g (0.15 mol) of isoamyl nitrite was dropwise addedthereto. Further, the mixture was refluxed for 12 hours and then cooled,and the salt was filtered. The organic layer was concentrated, andmethanol (500 ml) and 10% hydrochloric acid (20 ml) were added to theresidue, and the mixture was refluxed for one hour. After distilling offmethanol, water was added thereto, and the mixture was neutralized withan aqueous sodium hydrogencarbonate solution. The formed crystals werecollected by filtration to obtain 29.3 g (yield: 94.1%) of the desiredproduct. Melting point: 218°-220° C.

PREPARATION EXAMPLE 3-6 Preparation of methyl3-(t-butylaminosulfonyl)-1-methyl-1H-indazole-4-carboxylate and methyl3-(t-butylaminosulfonyl) 2-methyl-2H-indazole-4-carboxylate (compoundsrepresented by the formulas [I-d] and [II-d])

6.8 g (48 mmol) of methyl iodide was added to a solution containing 10 g(32 mmol) of the product from Preparation Example 3-5 and 6.6 g (48mmol) of potassium carbonate in methanol (200 ml), and the mixture wasrefluxed for 3 hours. Methanol was distilled off, and water was added tothe residue, and the mixture was extracted with ethyl acetate. Theorganic layer was washed with water, dried over anhydrous magnesiumsulfate, then concentrated and purified by silica gel columnchromatography to obtain 5.9 g (yield: 56.8%; melting point: 189°-190°C.) of methyl3-(t-butylaminosulfonyl)-1-methyl-1H-indazole-4-carboxylate and 2.1 g(yield: 19.8%; melting point: 147°-148° C.) of methyl3-(t-butylaminosulfonyl) 2-methyl-2H-indazole-4-carboxylate.

PREPARATION EXAMPLE 4 Preparation of 2-methyl-2H-indazole-3-sulfonamide(Intermediate No. 148)

A solution containing 9.5 g (72 mmol) of 2-methyl-2H-indazole in 200 mlof ethyl ether, was cooled to -30° C., and 61.4 g (144 mmol) of n-butyllithium (a 15% hexane solution) was dropwise added thereto. The mixturewas stirred for one hour at the same temperature, and then an excessamount of sulfurous acid gas was blown thereinto for 3 hours at atemperature of not higher than -20° C. After completion of the reaction,the mixture was returned to room temperature, stirred for 12 hours andthen diluted with ethyl ether. The product was subjected to filtration.The crystals were dried to obtain crude lithium2-methyl-2H-indazole-3-sulfinate. This product was used for thesubsequent reaction without purification. 48.8 g (430 mmol) ofhydroxylamine-O-sulfonic acid was gradually added to a solutioncontaining 17.2 g (430 mmol) of sodium hydroxide in water 300 ml) undercooling with ice (not higher than 10° C.). This solution was added allat once to a solution containing the crude lithium2-methyl-2H-indazole-3-sulfinate previously prepared in water (100 ml),and then the mixture was stirred for 12 hours at room temperature.Formed crystals were collected by filtration to obtain 8.8 g (yield:58%) of 2-methyl-2H-indazole-3-sulfonamide (slightly yellow granularcrystals). Melting point: 181°-183° C.

PREPARATION EXAMPLE 5 Preparation of1-(2-methyl-2H-indazole-3-sulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea(Compound No. II-23)

2.3 g (15 mmol) of DBU was added to a solution containing 3.2 g (15mmol) of 2-methyl-2H-indazole-3-sulfonamide obtained in PreparationExample 4 and 4.1 g (15 mmol) of phenyl(4,6-dimethoxypyrimidin-2-yl)carbamate in acetonitrile (50 ml), and themixture was stirred at room temperature for 12 hours. The mixture waspoured into ice water and acidified with citric acid. Formed crystalswere collected by filtration and washed with ice water, IPE and ethylether, to obtain 4.0 g (yield: 68%) of the desired product (colorlessneedle like crystals). Melting point: 199°-202° C.

PREPARATION EXAMPLE 6 Preparation of4-methoxy-1-methyl-1H-indazole-3-sulfonamide (Intermediate No. 65)

A solution containing 5 g (21.8 mmol) of 4-fluoro-1-methyl-1-indazole-3-sulfonamide and 12.6 g of sodium methoxide (a 28% methanolsolution) (65 mmol) in DMSO (50 ml), was stirred at 130° C. for onehour. After confirming the disappearance of the starting material bythin layer chromatography (TLC), the mixture was poured into ice waterand acidified with citric acid. Formed crystals were collected byfiltration and washed with water and IPE to obtain 3.2 g (yield: 60.9%)of the desired product. Melting point: 268°-270° C.

PREPARATION EXAMPLE 7 Preparation of4-ethylthio-2-methyl-2H-indazole-3-sulfonamide (Intermediate-No. 130)

4.8 g (77 mmol) of ethanethiol was added to a solution containing 8.6 g(77 mmol) of potassium t-butoxide in DMSO (70 ml), under cooling withice, and 8 g (35 mmol) of 4-fluoro-2-methyl-2H-indazole-3-sulfonamidewas further added thereto. This mixture was stirred at 120° C. for 2hours. After confirming the disappearance of the starting material byTLC, treatment was conducted in the same manner as in PreparationExample 6 to obtain 6.8 g (yield: 72.5%) of the desired product.Melting: 145°-147° C.

PREPARATION EXAMPLE 8-1 Preparation of4-cyclopropylmethoxy-2-methyl-2H-indazole-3-sulfonamide (IntermediateNo. 254)

2.8 g (70 mmol) of 60% sodium hydride was suspended in 50 ml of DMSO,and 6 g (83 mmol) of cyclopropane methanol was dropwise added thereto.The mixture was stirred at room temperature for one hour, and then 5.4 g(24 mmol) of 4-fluoro-2-methyl-2H-indazole-3-sulfonamide was addedthereto. The mixture was stirred at 130° C. for 3 hours. After thereaction, the mixture was poured into ice water, acidified with citricacid and extracted with ethyl acetate. The organic layer was washed withwater and then concentrated. Formed crystals were collected byfiltration, washed with IPE and then dried to obtain 5.8 g (yield: 90%)of the desired product. Melting point: 139°-141° C.

PREPARATION EXAMPLE 8-2 Preparation of4-hydroxy-2-methyl-2H-indazole-3-sulfonamide (Intermediate No. 189)

A mixture comprising 62 g (221 mmol) of4-cyclopropylmethoxy-2-methyl-2H-indazole-3-sulfonamide, 120 ml ofacetic acid and 120 ml of concentrated hydrochloric acid, was stirred at80° C. for one hour. After concentrating acetic acid-hydrochloric acid,the mixture was poured into ice water. Crystals were collected byfiltration and washed with water. Further, the crystals were washed withIPE and dried to obtain 35.1 g (yield: 70%) of the desired product.Melting point: 180°-181° C.

PREPARATION EXAMPLE 8-3 Preparation of4-allyloxy-2-methyl-2H-indazole-3-sulfonamide (Intermediate No. 203)

1.3 g of allyl bromide was added to a mixture comprising 5 g (22 mmol)of 4-hydroxy-2-methyl-2H-indazole-3-sulfonamide and 50 ml of a DMFsolution of 1.9 g (22 mmol) of sodium hydrogencarbonate, and the mixturewas stirred at room temperature for 12 hours. The mixture was pouredinto ice water, acidified with citric acid and extracted with ethylacetate. The organic layer was washed, then concentrated and purified bycolumn chromatography (hexane/ethyl acetate=2/1) to obtain 1.9 g (yield:32.5%) of the desired product. Melting point: 143°-144° C.

PREPARATION EXAMPLE 9 Preparation of4-(2-chloroethoxy-2-methyl-2H-indazole-3-sulfonamide (Intermediate No.229) (Mitsunobu reaction)

3.8 g (22 mmol) of diethylazo dicarboxylate was added to a solutioncontaining 5 g (22 mmol) of4-hydroxy-2-methyl-2H-indazole-3-sulfonamide, 1.8 g (22 mmol) of2-chloroethanol and 5.8 g (22 mmol) of triphenylphosphine in 50 ml ofTHF, and the mixture was stirred at room temperature for 20 hours. Themixture was poured into water and extracted with ethyl acetate. Theorganic layer was washed with water, then concentrated and purified bycolumn chromatography (hexane/ethyl acetate=2/1) to obtain 1.66 g(yield: 26%) of the desired product. Melting point: 177°-179° C.

PREPARATION EXAMPLE 10-1 Preparation of N¹, N¹ -dimethyl-N²-[(4-hydroxy-2-methyl-2H-indazol- 3-yl)sulfonyl]formamidine (compoundrepresented by the formula [II-i])

21.3 g (174 mmol) of dimethylformamide dimethylacetal was dropwise addedto a solution containing 33 g (145 mmol) of4-hydroxy-2-methyl-2H-indazole-3-sulfonamide in 200 ml of acetonitrile,at room temperature. The mixture was stirred for one hour, then pouredinto ice water and extracted with ethyl acetate. The organic layer waswashed with water, then concentrated and purified by columnchromatography to obtain 35.2 g (yield: 86.3%) of the desired product.Melting point: 118°-119° C.

PREPARATION EXAMPLE 10-2 Preparation of N¹,N-¹ -dimethyl-N²-{[4-(2-fluoroethoxy)-2-methyl-2H-indazol-3-yl]sulfonyl}formamidine(compound represented by the formula [II-j])

4.2 g (15 mmol) of N¹, N¹ -dimethyl-N²-[(4-hydroxy-2-methyl-2H-indazol-3-yl)sulfonyl]formamidine was added toa suspension containing 0.6 g (15 mmol) of 60% sodium hydride in 50 mlof DMF, and the mixture was stirred at room temperature for one hour.Further, 2 g (16 mmol) of 1-bromo-2-fluoroethane was added thereto, andthe mixture was stirred at room temperature for 12 hours. The mixturewas poured into ice water, and the formed crystals were collected byfiltration and washed with water and IPE to obtain the desired product.This product was used for the subsequent reaction without purification.Obtained amount: 3.4 g (yield: 69.5%)

PREPARATION EXAMPLE 10-3 Preparation of4-(2-fluoroethoxy)-2-methyl-2H-indazole-3-sulfonamide (Intermediate No.230)

A mixture comprising 3 4 g of N¹,N¹ -dimethyl-N²-([4-(2-fluoroethoxy)-2-methyl-2H-indazol-3-yl]sulfonyl}formamidine, 5ml of concentrated hydrochloric acid and 50 ml of ethanol, was refluxedfor 12 hours. Disappearance of the starting material was confirmed byTLC, and then ethanol was distilled off. Water was added to the residue,whereupon the formed crystals were collected by filtration and washedwith water and IPE to obtain 2.4 g (yield: 85%) of the desired product.Melting point: 178°-180° C.

PREPARATION EXAMPLE 11 Preparation of4-chloro-2-methyl-2H-indazole-3-sulfonamide (Intermediate No. 143)

36.1 g (0.24 mol) of 4-chloro-1H-indazole was added to a solutioncontaining 28.4 g (0.7 mol) of sodium hydroxide in 500 ml of methanol,and 85.2 g (0.6 mol) of methyl iodide was dropwise added thereto. Themixture was heated and refluxed for 4 hours. Then, methanol wasdistilled off, and water was added to the residue, followed byextraction with dichloromethane. The organic layer was washed withwater, dried and concentrated to obtain a mixture of4-chloro-1-methyl-1H-indazole and 4-chloro-2-methyl-2H-indazole. Thismixture was separated by silica gel column chromatography (ethylacetate/hexane= 4/1) to obtain 17.4 g (yield: 43.6%) of4-chloro-2-methyl-2H-indazole (yellow liquid, refractive index (20° C.):1.6095).

A solution containing 16 g (0.1 mol) of 4-chloro-2-methyl-2H-indazole in300 ml of ethyl ether, was cooled to -30° C., and 85.4 g (0.2 mol) ofn-butyl lithium (15% hexane solution) was dropwise added thereto. Themixture was stirred for one hour at the same temperature. Then, anexcess amount of sulfurous acid gas was blown thereinto at a temperatureof not higher than -20° C. for 3 hours. After completion of thereaction, the mixture was returned to room temperature and diluted withethyl ether, and the product was subjected to filtration. Crystals weredried to obtain crude lithium 4-chloro-2-methyl-2H-indazole-3-sulfinate.This product was used for the subsequent reaction without purification.

45.2 g (0.4 mol) of hydroxylamine-O-sulfonic acid was gradually added toa solution containing 16 g (0.4 mol) of sodium hydroxide in water (300ml) under cooling with ice (<10° C.). This solution was added all atonce to a solution of the previously prepared crude lithium4-chloro-2-methyl-2H-indazole-3-sulfinate in water (100 ml). The mixturewas stirred at room temperature for 12 hours. Formed crystals werecollected by filtration to obtain 17.1 g (yield: 69.8%) of the desired4-chloro-2-methyl-2H-indazole-3-sulfonamide (slightly yellow granularcrystals). Melting point: 173°-175° C.

PREPARATION EXAMPLE 12 Preparation of1-(4-chloro-2-methyl-2H-indazole-3-sulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea(Compound No. II-134)

0.5 g (3.3 mmol) of DBU was added to a solution containing 0.8 g (3.3mmol) of 4-chloro-2-methyl-2H-indazole-3-sulfonamide obtained inPreparation Example 11 and 0.9 g (3.3 mmol) of phenyl(4,6-dimethoxypyrimidin-2-yl)carbamate in acetonitrile (50 ml), and themixture was stirred at room temperature for 12 hours. The mixture waspoured into ice water and acidified with citric acid. Formed crystalswere collected by filtration and sequentially washed with water,isopropyl ether and ethyl ether, to obtain 1.2 g (yield: 85%) of thedesired product (colorless needle-like crystals). Melting point:171°-172° C.

The herbicide of the present invention contains an indazolesulfonylureaderivative represented by the general formula [I] or [II] as an activeingredient.

For the compound of the present invention to be used as a herbicide, thecompound of the present invention may be used by itself. However, it maybe used in the form of a formulation such as a dust, a wettable powder,an emulsifiable concentrate, a microgranule or a granule by blending itwith a carrier, a surfactant, a dispersant or an adjuvant which iscommonly used for formulations.

The carrier to be used for such formulations, may, for example, be asolid carrier such as Zeeklite, talc, bentonite, clay, kaolin,diatomaceous earth, fine silica, vermiculite, calcium carbonate, slakedlime, silica sand, ammonium sulfate or urea, or a liquid carrier such asisopropyl alcohol, xylene, cyclohexane or methylnaphthalene.

As the surfactant and dispersant, a metal salt of alkylbenzenesulfonicacid, a metal salt of dinaphthylmethane disulfonic acid, a salt ofalcohol-sulfuric acid ester, an alkylaryl sulfonate, a lignin sulfonate,a polyoxyethylene glycol ether, a polyoxyethylene alkylaryl ether or apolyoxyethylene sorbitol monoalkylate may, for example, be mentioned.

The adjuvant may, for example, be carboxymethyl cellulose, polyethyleneglycol or gum arabic.

In practical use, the herbicide may be diluted to a suitableconcentration before application, or may be directly applied.

The herbicide of the present invention may be used for application tofoliage, soil or water surface. The blending proportion of the activeingredient is suitably selected as the case requires. However, in a caseof a dust or a granule, the proportion of the active ingredient isselected suitably within a range of from 0.01 to 10% (by weight),preferably from 0.05 to 5% (by weight). In a case of an emulsifiableconcentrate or a wettable powder, the proportion is selected suitablywithin a range of from 1 to 50% (by weight), preferably from 5 to 30%(by weight).

The dose of the herbicide of the present invention varies depending uponthe type of the compound, the weeds to be controlled, the germinationtendency, the environmental conditions and the type of the formulationto be used. However, in the case of a dust or a granule which is used byitself, the dose of the active ingredient is selected suitably within arange of from 0.1 g to 5 kg, preferably from 1 g to 1 kg, per 10 ares.In a case of an emulsifiable concentrate or a wettable powder which isused in a liquid state, the dose of the active ingredient is selectedsuitably within a range of from 0.1 to 50,000 ppm, preferably from 10 to10,000 ppm.

Further, the compound of the present invention may be used incombination with an insecticide, a fungicide, other herbicide, a plantgrowth controlling agent, a fertilizer or the like, as the caserequires.

Now, the formulation method will be described with reference to typicalFormulation Examples. The compounds, types of the additives and blendingratios are not limited to such specific Examples and may be changedwithin wide ranges. In the following description, "parts" means "partsby weight".

FORMULATION EXAMPLE 1

(Wettable powder)

To 10 parts of Compound No. I-9 or II-26, 0.5 part ofpolyoxyethyleneoctylphenyl ether, 0.5 part of sodium β-naphthalenesulfonate-formalin condensate, 20 parts of diatomaceous earth and 69parts of clay were mixed and pulverized to obtain a wettable powder.

FORMULATION EXAMPLE 2

(Wettable powder)

To 10 parts of Compound No. I-63 or II-134, 0.5 part ofpolyoxyethyleneoctylphenyl ether, 0.5 part of sodium β-naphthalenesulfonate-formalin condensate, 20 parts of diatomaceous earth, 5 partsof fine silica and 64 parts of clay were mixed and pulverized to obtaina wettable powder.

FORMULATION EXAMPLE 3

(Wettable powder)

To 10 parts of Compound No. I-134 or II-104, 0.5 part ofpolyoxyethyleneoctylphenyl ether, 0.5 part of sodium β-naphthalenesulfonate-formalin condensate, 20 parts of diatomaceous earth, 5 partsof fine silica and 64 parts of calcium carbonate, were mixed andpulverized to obtain a wettable powder.

FORMULATION EXAMPLE 4

(Emulsifiable concentrate)

To parts of Compound No. I-92 or II-64, 60 parts of a mixture comprisingequal amounts of xylene and isophorone and 10 parts of a mixturecomprising a polyoxyethylene sorbitol alkylate surfactant, apolyoxyethylenealkylaryl polymer and an alkylaryl sulfonate, were added,and the mixture was thoroughly stirred to obtain an emulsifiableconcentrate.

FORMULATION EXAMPLE 5

(Granule)

10 Parts of Compound No. I-64 or II-142, 80 parts of a bulking agentcomprising a 1:3 mixture of talc and bentonite, 5 parts of fine silica,5 parts of a mixture comprising a polyoxyethylene sorbitol alkylatesurfactant, a polyoxyethylenealkylaryl polymer and an alkylarylsulfonate and 10 parts of water were mixed and thoroughly kneaded toobtain a paste, which was extruded from sieve apertures with a diameterof 0.7 mm. The extruded product was dried and then cut into a length offrom 0.5 to 1 mm to obtain granules.

The compound of the present invention represented by the general formula[I] or [II] is capable of controlling annual weeds such as barnyardgrass(Echinochloa oryzicola), smallflower umbrella-plant (Cyperus difformis)and monochoria (Monochoria vaginalis) as well as perennial weeds such asJapanese ribbon wapato (Sagittaria pygmaea), arrowhead (Sagittariatrifolia), water nutgrass (Cyperus serotinus), water chestnut(Eleocharis kuroguwai), bulrush (Scirpus juncoides) and narrow-leavedarrowhead (Alisma canaliculatum), which germinate in paddy fields.Further, it exhibits excellent herbicidal effects against various weedsproblematic in upland fields, including broadleaf weeds such assmartweed (Polygonum lapathifolium), green amaranth (Amaranthusviridis), lambsquater (Chenopodium album), goose grass (Galium aparine),chickweed (Stellaria media), velvetleaf (Abtilon theophrasti), pricklysida (Sida spinosa), hemp sesbania (Sesbania exaltata), morningglory(Ipomoea spp) and common cocklebur (Xanthium strumarium), perennial andannual syperaceous weeds such as purple nutsedge (Cyperus rotundus),yellow nutsedge (Cyperus esculentus), himekugu (Cyperus brevifolius var.leiolepis), annual sedge (Cyperus microiria) and rice flatsedge (Cyperusiria), and gramineous weeds such as barnyardgrass (Echinochloacrus-galli), goosegrass (Eleusine indica), greenfoxtail (Setariaviridis), annual bluegrass (Poa annua), johnsongrass (Sorghumhalepense), water foxtail (Alopecurus aequalis) and wild oat (Avenafatua), over a wide range from the preemergence stage to the growingstage.

On the other hand, the herbicide of the present invention is highly safeto crop plants and exhibits particularly high safety to e.g. rice,wheat, barley, corn, grain sorghum and sugar beat.

Now, the effects of the compounds of the present invention will bedescribed with reference to Test Examples.

TEST EXAMPLE 1

(Test on herbicidal effects by paddy field soil treatment)

In a plastic pot (surface area: 100 cm²) filled with paddy field soil,barnyardgrass (Ec), monochoria (Mo) and bulrush (Sc) were sown afterpuddling and leveling, and flooded to a water depth of 3 cm. Next day, awettable powder prepared in accordance with Formulation Example 1 wasdiluted with water and applied dropwise to the water surface. The dosewas 100 g of the active ingredient per 10 ares. The plants were thencultured in a green house, and the evaluation of the herbicidal effectswas conducted on the 21st day after the application in accordance withthe standards as identified in Table 4. The results are shown in Table5.

                  TABLE 4                                                         ______________________________________                                                     Herbicidal effects                                               Index        (growth-controlling degree)                                      No.          or phytotoxicity                                                 ______________________________________                                        5            Herbicidal effect or phytotoxicity:                                           at least 90%                                                     4            Herbicidal effect or phytotoxicity:                                           at least 70% and less than 90%                                   3            Herbicidal effect or phytotoxicity:                                           at least 50% and less than 70%                                   2            Herbicidal effect or phytotoxicity:                                           at least 30% and less than 50%                                   1            Herbicidal effect or phytotoxicity:                                           at least 10 and less than 30%                                    0            Herbicidal effect or phytotoxicity:                                           0 to less than 10%                                               ______________________________________                                    

                  TABLE 5                                                         ______________________________________                                        Compound   Herbicidal effects                                                 No.        Ec            Mo     Sc                                            ______________________________________                                        I-5        5             5      5                                             I-6        5             5      5                                             I-8        5             5      5                                             I-17       5             5      5                                             I-18       5             5      5                                             I-19       5             5      5                                             I-20       5             5      5                                             I-23       5             5      5                                             I-25       5             5      5                                             I-26       5             5      5                                             I-27       5             5      5                                             I-28       5             5      5                                             I-29       5             5      5                                             I-31       5             5      5                                             I-32       5             5      5                                             I-33       5             5      5                                             I-34       5             5      5                                             I-35       5             5      5                                             I-63       5             5      5                                             I-64       5             5      5                                             I-65       5             5      5                                             I-66       5             5      5                                             I-67       5             5      5                                             I-79       5             5      5                                             I-91       5             5      5                                             I-92       5             5      5                                             I-93       5             5      5                                             I-94       5             5      5                                             I-95       5             5      5                                             I-111      5             5      5                                             I-114      5             5      5                                             I-120      5             5      5                                             I-131      5             5      5                                             I-134      5             5      5                                             I-136      3             5      5                                             I-149      5             5      4                                             I-150      5             5      5                                             I-151      5             5      4                                             I-153      5             5      5                                             I-157      5             5      5                                             I-158      5             5      5                                             I-160      5             5      5                                             I-161      5             5      5                                             I-162      5             5      5                                             I-174      5             5      5                                             I-175      5             5      5                                             I-176      5             5      5                                             I-179      5             5      5                                             I-180      5             5      5                                             I-181      5             5      5                                             I-182      5             5      5                                             I-183      5             5      5                                             I-184      5             5      5                                             I-194      5             5      5                                             I-204      5             5      5                                             I-205      5             5      5                                             I-216      5             5      5                                             I-218      5             5      4                                             I-322      5             5      5                                             I-334      5             5      5                                             I-337      5             5      5                                             I-506      5             5      5                                             I-507      5             5      5                                             I-508      4             5      4                                             I-513      3             5      5                                             I-514      5             5      5                                             I-516      5             5      5                                             I-517      5             5      5                                             I-518      5             5      5                                             I-519      5             5      4                                             I-520      3             5      5                                             I-527      3             5      5                                             I-530      5             5      5                                             I-555      5             5      4                                             I-641      5             5      5                                             I-645      3             5      5                                             I-906      3             5      5                                             II-5       5             5      5                                             II-6       5             5      5                                             II-8       5             5      5                                             II-17      5             5      5                                             II-18      4             5      4                                             II-19      5             5      5                                             II-20      5             5      5                                             II-23      5             5      5                                             II-25      5             5      5                                             II-26      5             5      5                                             II-27      5             5      5                                             II-28      5             5      5                                             II-29      5             5      5                                             II-31      5             5      5                                             II-32      5             5      5                                             II-33      5             5      5                                             II-34      5             5      5                                             II-35      5             5      5                                             II-36      5             5      5                                             II-38      5             5      5                                             II-42      4             5      5                                             II-53      5             5      5                                             II-55      6             5      5                                             II-63      5             5      5                                             II-64      5             5      5                                             II-65      5             5      5                                             II-66      5             5      5                                             II-67      5             5      5                                             II-91      5             5      5                                             II-92      5             5      5                                             II-93      5             5      5                                             II-94      5             5      5                                             II-95      5             5      5                                             II-104     5             5      5                                             II-106     5             5      5                                             II-107     5             5      5                                             II-110     5             5      5                                             II-111     5             5      5                                             II-112     5             5      5                                             II-113     5             5      5                                             II-114     5             5      5                                             II-115     5             5      5                                             II-120     5             5      5                                             II-127     5             5      5                                             II-129     4             5      5                                             II-130     5             5      5                                             II-131     5             5      5                                             II-132     3             5      5                                             II-134     5             5      5                                             II-136     3             5      5                                             II-137     5             5      5                                             II-141     5             5      5                                             II-142     5             5      5                                             II-143     5             5      5                                             II-149     5             5      5                                             II-150     5             5      5                                             II-151     5             5      5                                             II-153     5             5      5                                             II-155     5             5      5                                             II-156     5             5      5                                             II-157     5             5      5                                             II-158     5             5      5                                             II-159     5             5      5                                             II-160     5             5      5                                             II-161     5             5      5                                             II-162     5             5      5                                             II-163     5             5      5                                             II-166     5             5      5                                             II-168     5             5      5                                             II-169     5             5      5                                             II-174     5             5      5                                             II-175     5             5      5                                             II-176     5             5      5                                             II-177     5             5      5                                             II-178     5             5      5                                             II-179     5             5      5                                             II-180     5             5      5                                             II-181     5             5      5                                             II-182     5             5      5                                             II-183     5             5      5                                             II-184     5             5      5                                             II-185     5             5      5                                             II-188     5             5      5                                             II-189     5             5      5                                             II-194     5             5      5                                             II-195     5             5      5                                             II-197     5             5      5                                             II-198     5             5      5                                             II-199     5             5      5                                             II-200     5             5      5                                             II-202     4             5      5                                             II-204     5             5      5                                             II-208     5             5      5                                             II-215     5             5      5                                             II-220     5             5      5                                             II-225     5             5      5                                             II-227     5             5      5                                             II-531     5             5      5                                             ______________________________________                                    

TEST EXAMPLE 2 (Test on herbicidal effects by upland field soiltreatment)

In a plastic pot (surface area: 120 cm²) filled with upland field soil,pale smartweed (Po), slender amaranth (Am), common lambsquarters (Ch)and rice flatsedge (Ci) were sown and covered with soil. A wettablepowder prepared in accordance with Formulation Example 1 was dilutedwith water and applied uniformly to the soil surface by a small-sizedsprayer in an amount of 100 l/10 ares so as to apply 100 g of the activeingredient per 10 ares. The plants were then cultured in a green house,and the evaluation of the herbicidal effects was conducted on the 21stday after the application in accordance with the standards as identifiedin Table 4. The results are shown in Table 6.

                  TABLE 6                                                         ______________________________________                                        Compound     Herbicidal effects                                               No.          Po     Am         Ch   Ci                                        ______________________________________                                        I-5          5      5          5    5                                         I-6          5      5          5    5                                         I-8          5      5          5    5                                         I-17         5      5          5    5                                         I-18         5      5          5    5                                         I-19         5      5          5    5                                         I-20         5      5          5    5                                         I-23         5      5          5    --                                        I-25         5      5          5    --                                        I-26         5      5          5    5                                         I-27         5      5          5    5                                         I-28         5      5          5    --                                        I-29         5      5          5    --                                        I-31         5      5          5    5                                         I-32         5      5          5    5                                         I-33         5      5          5    5                                         I-34         5      5          5    5                                         I-35         5      5          5    5                                         I-53         5      5          5    5                                         I-63         5      5          5    5                                         I-64         5      5          5    5                                         I-65         5      5          5    5                                         I-66         5      5          5    5                                         I-67         5      5          5    5                                         I-79         5      5          5    5                                         I-91         5      5          5    5                                         I-92         5      5          5    5                                         I-93         5      5          5    5                                         I-94         5      5          5    5                                         I-95         5      5          5    5                                         I-110        5      5          5    5                                         I-111        5      5          5    5                                         I-112        5      5          5    5                                         I-113        5      5          5    5                                         I-114        5      5          5    5                                         I-120        5      5          5    5                                         I-131        5      5          5    5                                         I-134        5      5          5    5                                         I-136        5      5          5    5                                         I-149        5      5          5    5                                         I-150        5      5          5    5                                         I-151        5      5          5    5                                         I-152        5      5          4    5                                         I-153        5      5          5    5                                         I-157        5      5          5    5                                         I-158        5      5          5    5                                         I-160        5      5          5    5                                         I-161        5      5          5    5                                         I-162        5      5          5    5                                         I-174        5      5          5    5                                         I-175        5      5          5    5                                         I-176        5      5          5    --                                        I-177        5      5          5    --                                        I-178        5      5          5    5                                         I-179        5      5          5    --                                        I-180        5      5          5    5                                         I-181        5      5          5    5                                         I-182        5      5          5    5                                         I-183        5      5          4    5                                         I-184        5      5          4    5                                         I-194        5      5          5    5                                         I-198        5      5          5    5                                         I-199        5      5          5    5                                         I-204        5      5          5    5                                         I-205        5      5          4    5                                         I-209        5      5          4    5                                         I-212        5      5          5    5                                         I-216        5      5          5    5                                         I-218        4      5          4    5                                         I-322        5      5          5    --                                        I-334        5      5          5    --                                        I-337        5      5          5    --                                        I-506        5      5          5    5                                         I-507        5      5          5    5                                         I-508        5      5          5    5                                         I-509        5      5          4    5                                         I-511        5      5          5    4                                         I-513        5      5          5    5                                         I-514        5      5          5    4                                         I-516        5      5          5    5                                         I-517        4      5          4    5                                         I-518        5      5          5    5                                         I-519        5      5          5    5                                         I-520        5      5          5    5                                         I-521        5      5          5    5                                         I-525        5      5          5    5                                         I-526        4      5          4    5                                         I-527        5      5          5    5                                         I-528        5      5          5    5                                         I-529        4      5          5    5                                         I-530        5      5          5    5                                         I-555        5      5          5    5                                         I-641        5      5          5    5                                         I-761        4      5          4    --                                        I-905        5      5          5    --                                        I-906        5      5          5    --                                        II-5         5      5          5    5                                         II-6         5      5          4    5                                         II-8         5      5          5    5                                         II-17        5      5          5    5                                         II-19        5      5          5    5                                         II-20        5      5          5    5                                         II-23        5      5          5    5                                         II-25        5      5          4    5                                         II-26        5      5          5    5                                         II-27        5      5          5    5                                         II-28        5      5          5    5                                         II-29        5      5          5    --                                        II-31        5      5          5    5                                         II-32        5      5          5    5                                         II-34        5      5          5    5                                         II-35        5      5          5    5                                         II-36        5      5          5    5                                         II-38        5      5          4    5                                         II-53        5      5          5    --                                        II-55        5      5          4    5                                         II-56        5      5          5    5                                         II-63        5      5          5    5                                         II-64        5      5          5    5                                         II-65        5      5          5    --                                        II-66        5      5          5    --                                        II-67        5      5          5    --                                        II-90        4      5          5    --                                        II-91        5      5          5    5                                         II-92        5      5          5    5                                         II-93        5      5          4    5                                         II-95        4      5          4    5                                         II-96        5      5          4    5                                         II-104       5      5          5    --                                        II-105       4      5          5    --                                        II-106       5      5          5    5                                         II-107       5      5          5    5                                         II-110       5      5          5    5                                         II-111       5      5          5    5                                         II-113       5      5          5    5                                         II-114       5      5          5    5                                         II-115       5      5          4    4                                         II-120       5      5          5    5                                         II-127       5      5          5    5                                         II-130       5      5          4    5                                         II-131       5      5          5    5                                         II-134       5      5          5    5                                         II-136       5      5          5    5                                         II-137       5      5          5    --                                        II-138       5      5          5    --                                        II-139       5      5          5    --                                        II-140       5      5          4    --                                        II-141       5      5          5    --                                        II-142       5      5          5    --                                        II-143       5      5          5    --                                        II-144       5      5          5    --                                        II-145       5      5          5    --                                        II-146       5      5          5    5                                         II-149       5      5          4    5                                         II-150       5      5          5    5                                         II-155       5      5          5    5                                         II-156       4      5          5    5                                         II-157       5      5          5    5                                         II-158       5      5          5    5                                         II-160       5      5          5    5                                         II-161       4      5          4    5                                         II-162       5      5          5    5                                         II-163       5      5          4    5                                         II-164       5      5          5    5                                         II-166       5      5          5    5                                         II-167       4      5          5    5                                         II-168       5      5          5    5                                         II-169       5      5          5    5                                         II-170       4      5          5    5                                         II-172       5      5          5    5                                         II-174       5      5          5    5                                         II-175       5      5          5    --                                        II-176       5      5          5    --                                        II-177       5      5          5    --                                        II-178       5      5          5    --                                        II-179       5      5          5    --                                        II-180       5      5          5    5                                         II-181       5      5          5    5                                         II-182       5      5          5    5                                         II-183       5      5          4    5                                         II-184       5      5          5    5                                         II-185       5      5          5    5                                         II-188       5      5          5    5                                         II-189       5      5          5    5                                         II-191       5      5          5    --                                        II-195       5      5          5    4                                         II-197       5      5          5    --                                        II-198       5      5          5    --                                        II-199       5      5          5    --                                        II-200       5      5          5    --                                        II-204       5      5          4    5                                         II-207       5      5          4    --                                        II-219       4      5          5    5                                         II-220       5      5          5    --                                        II-223       5      5          5    --                                        II-225       5      5          5    5                                         II-226       5      5          5    5                                         II-227       5      5          5    --                                        II-531       5      5          5    --                                        ______________________________________                                    

EXAMPLE 3 (Test on herbicidal effects by upland field foliage treatment)

In a plastic pot (surface area: 120 cm²) filled with upland field soil,pale smartweed (Po), slender amaranth (Am), common lambsquarters (Ch)and rice flatsedge (Ci) were sown and covered with soil and werecultured in a green house for 2 weeks. A wettable powder prepared inaccordance with Formulation Example 1 was diluted with water and appliedonto the entire foliages of the plants from above by a small-sizedsprayer in an amount of 100 l/10 ares so as to apply 100 g of the activeingredient per 10 ares. The plants were then cultured in the greenhouse, and the evaluation of the herbicidal effects was conducted on the14th day after the treatment in accordance with the standards asidentified in Table 4. The results are shown in Table 7.

                  TABLE 7                                                         ______________________________________                                        Compound     Herbicidal effects                                               No.          Po     Am         Ch   Ci                                        ______________________________________                                        I-5          5      5          5    5                                         I-6          5      5          5    5                                         I-8          5      5          5    5                                         I-17         5      5          5    5                                         I-18         5      5          5    5                                         I-19         5      5          5    5                                         I-20         5      5          5    5                                         I-23         5      5          5    5                                         I-25         5      5          5    5                                         I-26         5      5          5    5                                         I-27         5      5          5    5                                         I-28         5      5          5    5                                         I-29         5      5          5    5                                         I-31         5      5          5    5                                         I-32         5      5          5    5                                         I-33         5      5          5    5                                         I-34         5      5          5    5                                         I-35         5      5          5    5                                         I-53         5      5          5    5                                         I-63         5      5          5    5                                         I-64         5      5          5    5                                         I-65         5      5          5    5                                         I-66         5      5          5    5                                         I-67         5      5          5    5                                         I-79         5      5          5    5                                         I-91         5      5          5    5                                         I-92         5      5          5    5                                         I-93         5      5          5    5                                         I-94         5      5          5    5                                         I-95         5      5          5    5                                         I-111        5      5          5    5                                         I-112        5      5          5    5                                         I-113        5      5          5    5                                         I-114        5      5          5    5                                         I-120        5      5          5    5                                         I-131        5      5          5    5                                         I-134        5      5          5    5                                         I-136        5      5          4    4                                         I-149        4      5          4    5                                         I-150        5      5          5    5                                         I-151        5      5          5    5                                         I-157        5      5          5    5                                         I-158        5      5          5    5                                         I-160        5      5          5    5                                         I-161        5      5          5    5                                         I-162        5      5          5    5                                         I-174        5      5          5    5                                         I-175        5      5          5    5                                         I-176        5      5          5    5                                         I-177        4      4          5    5                                         I-178        5      5          5    5                                         I-179        5      5          5    5                                         I-180        5      5          5    5                                         I-181        5      5          5    5                                         I-182        5      5          5    5                                         I-183        5      5          5    4                                         I-184        5      5          5    5                                         I-194        5      5          5    5                                         I-204        5      5          5    5                                         I-205        5      5          5    5                                         I-206        5      5          5    4                                         I-209        4      5          5    4                                         I-211        4      5          5    4                                         I-212        4      5          5    4                                         I-216        5      5          5    5                                         I-218        5      5          4    4                                         I-322        5      5          5    5                                         I-324        4      5          4    5                                         I-334        5      5          4    5                                         I-337        5      5          5    5                                         I-506        4      5          4    5                                         I-507        5      5          5    5                                         I-508        5      5          5    5                                         I-509        5      5          5    5                                         I-511        4      5          5    4                                         I-513        5      5          5    5                                         I-514        5      5          5    4                                         I-516        5      5          5    5                                         I-517        5      5          4    5                                         I-518        5      5          5    5                                         I-520        5      5          5    5                                         I-525        5      5          5    5                                         I-526        5      5          5    4                                         I-527        5      5          5    5                                         I-528        5      5          5    5                                         I-530        5      5          5    5                                         I-555        5      5          5    5                                         I-641        5      5          5    5                                         II-5         5      5          5    5                                         II-6         4      5          5    5                                         II-8         5      5          4    5                                         II-17        5      5          4    5                                         II-19        5      5          5    5                                         II-20        5      5          5    5                                         II-23        5      5          5    5                                         II-25        5      5          5    5                                         II-26        5      5          5    5                                         II-27        5      5          5    5                                         II-28        5      5          5    5                                         II-29        5      5          5    5                                         II-31        5      5          4    5                                         II-32        5      5          5    5                                         II-34        5      5          5    5                                         II-35        5      5          5    5                                         II-38        5      5          4    5                                         II-53        5      5          5    5                                         II-55        5      5          5    5                                         II-56        5      5          5    5                                         II-63        5      5          5    5                                         II-64        5      5          5    5                                         II-65        5      5          5    5                                         II-66        5      5          5    5                                         II-67        5      5          5    5                                         II-91        5      5          5    5                                         II-92        5      5          5    5                                         II-93        5      5          5    5                                         II-94        5      5          5    5                                         II-104       5      5          5    5                                         II-105       5      5          5    5                                         II-106       5      5          5    5                                         II-107       5      5          5    5                                         II-110       5      5          5    5                                         II-111       5      5          5    5                                         II-112       5      5          5    5                                         II-113       5      5          5    5                                         II-114       5      5          5    5                                         II-115       5      5          4    5                                         II-120       5      5          5    5                                         II-129       5      5          5    5                                         II-130       5      5          5    5                                         II-131       5      5          5    5                                         II-134       5      5          5    5                                         II-136       5      5          4    4                                         II-140       5      5          5    5                                         II-141       4      5          4    5                                         II-142       5      5          5    5                                         II-143       5      5          5    5                                         II-146       5      5          4    5                                         II-149       5      5          5    5                                         II-150       5      5          5    5                                         II-153       5      5          4    4                                         II-154       5      5          5    4                                         II-155       5      5          5    5                                         II-157       5      5          5    5                                         II-158       5      5          4    5                                         II-160       5      5          5    5                                         II-162       5      5          5    5                                         II-166       5      5          5    5                                         II-167       5      5          5    5                                         II-168       5      5          5    5                                         II-169       5      5          5    5                                         II-170       4      5          5    5                                         II-174       5      5          4    5                                         II-175       5      5          4    5                                         II-176       5      4          5    5                                         II-178       5      5          5    5                                         II-179       5      5          5    5                                         II-180       5      5          5    5                                         II-181       5      5          5    5                                         II-182       5      5          5    5                                         II-183       5      5          4    5                                         II-184       5      5          5    5                                         II-188       5      5          5    5                                         II-189       5      5          4    5                                         II-192       4      5          4    5                                         II-194       5      5          5    5                                         II-195       5      5          5    5                                         II-196       4      5          4    5                                         II-197       5      5          5    5                                         II-199       5      5          5    5                                         II-204       5      5          5    5                                         II-218       5      5          5    4                                         II-219       4      5          5    4                                         II-220       5      5          4    5                                         II-225       5      5          5    5                                         II-226       5      5          5    5                                         II-531       5      5          5    5                                         ______________________________________                                    

TEST EXAMPLE 4

(Test on crop plant selectivity by paddy field soil treatment)

In a 1/10,000a plastic pot, paddy field soil was filled, irrigated,paddled and leveled. Then, barnyardgrass (Ec), monochoria (Mo) andbulrush (Sc) were sown at a depth of 0.5 cm. Further, two seedlings ofrice (Or) of 2 leaf stage was transplanted at a transplantation depth of2 cm. Then, the pot was flooded to a water depth of 3 cm. Next day, aprescribed amount of the active ingredient (g^(ai) /10a) of a wettablepowder prepared in accordance with Formulation Example 1 was dilutedwith water and applied dropwise to the water surface. The plants werethen cultured in a green house, and the evaluation of the herbicidaleffects and phytotoxicity was conducted on the 28th day after theapplication in accordance with the standards as identified in Table 4.The results are shown in Table 8.

                  TABLE 8                                                         ______________________________________                                        Compound                                                                              Dose       Herbicidal effects                                                                          Phytotoxicity                                No.     (gai 10a)  Eo     Mo    Sc   Or                                       ______________________________________                                        I-17    25         4      5     5    0                                        I-157   6.3        5      5     5    1                                        I-161   25         5      5     5    0                                        I-174   25         5      5     4    1                                        I-216   25         4      5     4    2                                        II-19   25         5      5     5    0                                                6.3        5      5     5    0                                        II-23   25         4      5     5    0                                        II-26   25         5      5     5    1                                                6.3        5      5     5    0                                                1.6        5      5     4    0                                        II-27   25         5      5     5    0                                                6.3        5      5     5    0                                        II-29   6.3        5      5     5    1                                                1.6        3      5     5    0                                        II-31   6.3        5      5     5    1                                                1.6        5      5     5    0                                        II-35   25         5      5     5    1                                                6.3        5      5     5    0                                        II-36   25         5      5     5    0                                        II-53   25         5      5     5    0                                        II-64   25         5      5     5    0                                                6.3        5      5     5    0                                        II-65   25         5      5     5    0                                                6.3        5      5     5    0                                        II-66   25         5      5     5    1                                                6.3        5      5     5    0                                        II-92   25         5      5     5    2                                                6.3        5      5     5    0                                                1.6        5      5     5    0                                        II-93   25         5      5     5    1                                                6.3        5      5     5    0                                        II-94   25         5      5     5    1                                                6.3        5      5     5    0                                        II-104  25         5      5     5    0                                                6.3        5      5     5    0                                        II-114  6.3        5      5     5    1                                                1.6        5      5     5    0                                        II-127  25         5      5     5    1                                                6.3        3      5     5    0                                        II-134  25         5      5     5    0                                                6.3        5      5     5    0                                        II-137  25         5      5     5    2                                                6.3        5      5     5    0                                                1.6        5      5     5    0                                        II-141  25         5      5     5    1                                                6.3        5      5     4    0                                        II-142  6.3        5      5     5    0                                                1.6        5      5     5    0                                        II-157  25         5      5     5    0                                                6.3        5      5     5    0                                        II-160  25         5      5     5    0                                                6.3        5      5     5    0                                        II-162  25         5      5     5    1                                                6.3        5      5     5    0                                        II-166  1.6        5      5     5    0                                        II-178  25         5      5     5    0                                                6.3        4      5     4    0                                        II-208  25         5      5     5    0                                                6.3        4      5     4    0                                        II-531  25         5      5     5    0                                                6.3        5      5     4    0                                        Compar- 25         5      5     5    5                                        ative   6.3        5      5     4    5                                        compound                                                                              1.6        3      4     2    5                                        ______________________________________                                         Comparative compound A: Disclosed in Japanese Unexamined Patent               Publication No. 95091/1992 (Compound No. 1)                              

TEST EXAMPLE 5

(Test on crop plant selectivity by upland field soil treatment)

In a plastic pot (surface area: 600 cm²) filled with upland field soil,seedsor tubers of wheat (Tr), corn (Ze), grain sorghum (Gs), palesmartweed (Po), slender amaranth (Am), common lambsquarters (Ch),velvetleaf (Ab), morningglory (Ip), cocklebur (Xa) and purple nutsedge(CR) were planted and covered with soil. Next day, a prescribed amountof the active ingredient (g^(ai) /10a) of a wettable powder prepared inaccordance with Formulation Example 1 was diluted with water and applieduniformly to the soil surface by a small-sized sprayer in an amount of100 l per 10 ares. The plants were then cultured in a green house, andthe evaluation of the herbicidal effects was conducted on the 21st dayafter the application in accordance with the standards as identified inTable 4. The results are shown in Table 9.

                  TABLE 9                                                         ______________________________________                                        Com-           Herbicidal          Phyto-                                     pound Dose     effects             toxicity                                   No.   (gai 10a)                                                                              Po    Am   Ch  Ab  Ip  Xa  CR   Tr  Ze  Gs                     ______________________________________                                        II-19 25       5     5    5   5   5   5   2    0   1   0                      II-23 25       5     5    5   5   5 5 5   0    3   1                                6.3      4     5    4   5   4   5   5    0   3   0                      II-26 25       5     5    5   5   5   5   --   1   4   3                            6.3      5     5    4   4   4   4   4    0   3   1                      II-28 25       5     5    5   5   5   5   --   0   1   0                            6.3      5     5    4   4   4   4   4    0   0   0                      II-29 25       5     5    5   5   5   5   5    0   3   3                            6.3      5     5    5   5   5   5   5    0   1   1                      II-35 6.3      5     5    5   4   4   4   5    0   1   0                      II-53 25       5     5    5   5   5   5   5    1   2   1                            6.3      5     5    5   5   5   5   4    0   0   0                      II-63 25       5     5    5   5   5   5   5    0   5   3                            6.3      5     5    5   5   5   5   5    0   3   2                      II-64 6.3      5     5    5   5   5   5   5    0   1   3                            1.6      5     5    5   3   5   5   5    0   0   0                      II-65 25       5     5    5   5   5   5   5    1   1   4                            6.3      5     5    5   4   4   5   5    0   0   3                      II-66 25       5     5    5   5   5   5   5    0   4   4                            6.3      5     5    5   5   4   5   5    0   1   3                      II-91 6.3      5     5    5   5   5   5   5    0   4   1                      II-104                                                                              25       5     5    5   5   5   5   5    0   4   3                            6.3      5     5    5   4   4   5   5    0   1   3                      II-107                                                                              25       5     5    5   5   5   5   5    0   4   4                            6.3      5     5    5   4   3   5   5    0   3   3                      II-134                                                                              25       5     5    5   5   5   5   5    1   1   1                            6.3      5     5    5   5   5   5   5    0   0   0                      II-137                                                                              25       5     5    5   5   5   5   5    0   4   2                            6.3      5     5    5   5   4   5   5    0   3   1                      II-142                                                                              25       5     5    5   5   5   5   5    1   4   4                            6.3      5     5    5   5   5   5   5    0   3   3                      II-157                                                                              25       5     5    5   5   5   5   4    2   4   0                            6.3      5     5    5   5   3   5   3    0   1   0                      II-168                                                                              25       5     5    5   5   5   5   4    1   4   4                            6.3      5     5    5   4   4   5   3    0   3   3                      II-215                                                                              25       5     5    5   4   5   5   5    1   2   1                      ______________________________________                                    

TEST EXAMPLE 5

(Test on crop plant selectivity by upland field foliage treatment)

In a plastic pot (surface area: 600 cm²) filled with upland field soil,seeds or tubers of wheat (Tr), corn (Ze), grain sorghum (Gs), palesmartweed (Po), slender amaranth (Am), common lambsquarters (Ch),velvetleaf (Ab), morningglory (Ip), cocklebur (Xa) and purple nutsedge(CR) were planted, covered with soil and cultured in a green house for 2weeks. Then, a prescribed amount of the active ingredient (g^(ai) /10a)of a wettable powder prepared in accordance with Formulation Example 1was diluted with water and applied onto the entire foliages of theplants from above by a small-sized sprayer in an amount of 100 l per 10ares. The plants were then cultured in a green house, and the evaluationof the herbicidal effects was conducted on the 14th day after thetreatment in accordance with the standards as identified in Table 4. Theresults are shown in Table 10.

                  TABLE 10                                                        ______________________________________                                        Com-           Herbicidal          Phyto-                                     pound Dose     effects             toxicity                                   No.   (gai 10a)                                                                              Po    Am   Ch  Ab  Ip  Xa  CR   Tr  Ze  Gs                     ______________________________________                                        I-20  6.3      5     5    5   5   5   5   3    1   3   3                      I-23  25       5     5    5   5   5   5   2    0   4   3                            6.3      5     5    5   5   5   5   0    0   3   3                      I-26  1.6      5     5    5   5   5   5   5    1   4   4                      I-27  6.3      5     5    5   5   5   5   3    1   3   3                            1.6      5     5    4   5   5   5   1    0   3   3                      I-28  25       5     5    5   3   5   5   2    1   3   3                            6.3      5     5    4   5   4   5   1    0   3   3                      I-53  25       5     5    5   5   5   5   3    1   3   3                            6.3      5     5    5   5   5   5   1    0   3   2                      I-66  6.3      5     5    5   5   5   5   2    1   3   --                     I-176 25       5     5    5   5   5   5   3    1   3   3                            6.3      5     5    5   5   5   4   2    0   3   3                      I-194 25       5     5    4   5   5   5   3    0   4   4                      I-204 25       5     5    4   5   5   5   --   1   4   4                            6.3      4     5    4   5   5   5   --   0   4   3                      I-337 25       5     5    5   5   5   5   4    1   4   3                            6.3      4     5    5   5   5   5   4    0   3   3                      I-516 25       4     5    5   5   5   5   2    0   4   3                      II-20 25       5     5    5   5   5   5   5    0   4   3                            6.3      5     5    5   5   5   5   5    0   4   3                      II-26 25       5     5    5   5   5   5   5    0   3   1                            6.3      5     5    5   5   5   5   5    0   2   1                      II-27 25       5     5    5   5   5   5   2    0   0   0                            6.3      5     5    5   5   5   5   1    0   0   0                      II-28 25       5     5    5   5   5   5   5    1   3   3                            6.3      5     5    5   5   5   5   5    0   2   2                      II-31 25       5     5    5   5   5   5   5    1   1   1                            6.3      5     5    4   5   5   5   5    0   1   1                      II-64 25       5     5    5   5   5   5   4    0   0   3                            6.3      5     5    5   5   5   5   4    0   0   2                      II-93 25       5     5    5   5   5   5   5    1   1   3                            6.3      5     5    5   5   5   5   5    0   1   3                      II-104                                                                              100      5     5    5   5   5   5   5    0   0   3                            25       5     5    5   5   5   5   4    0   0   3                      II-127                                                                              25       5     5    4   5   5   5   5    0   4   1                      II-134                                                                              25       5     5    5   5   5   5   5    0   0   0                            6.3      5     5    4   5   5   5   5    0   0   0                      II-150                                                                              25       5     5    4   5   5   5   --   0   1   3                      II-157                                                                              25       5     5    5   5   5   5   --   0   0   2                            6.3      5     5    4   5   5   5   --   0   0   1                      II-168                                                                              25       5     5    5   5   5   5   4    1   4   3                            6.3      5     5    4   5   5   5   3    0   2   3                      II-180                                                                              25       5     5    5   5   5   5   --   0   0   1                            6.3      5     5    4   5   5   5   --   0   0   1                      II-181                                                                              25       5     5    5   5   5   5   5    1   3   2                            6.3      5     5    5   5   5   5   4    0   1   1                      ______________________________________                                    

We claim:
 1. An indazolesulfonylurea derivative of the formula:##STR79## wherein R¹ is a hydrogen atom, a straight or branched chainC₁₋₃₀ alkyl group, a C₃ cycloalkyl group, a C₁₋₃₀ haloalkyl group, aC₁₋₃₀ haloalkyl group, a C₁₋₃₀ alkoxyalkyl group, a C₁₋₃₀ benzyloxyalkylgroup, a benzyl group, a phenyl group, a pyridyl group, a C₁₋₃₀dialkylaminocarbonyl group, a C₁₋₃₀ alkoxycarbonyl group, a C₁₋₃₀alkylsulfonyl group, a phenylsulfonyl group, a C₁₋₃₀dialkylaminosulfonyl group, a C₁₋₃₀ haloalkylcarbonyl group, a C₁₋₃₀alkylcarbonyl group, a benzoyl group or a C₂₋₂₀ alkenyl group;R² and R³are, independently, a hydrogen atom, a halogen atom, a straight orbranched chain C₁₋₃₀ alkyl group, a C₃ cycloalkyl group, a C₂₋₂₀ alkenylgroup, a C₁₋₃₀ alkoxycarbonylalkenyl group, a C₂₋₂₀ alkynyl group, aC₁₋₃₀ haloalkyl group, an C₁₋₃₀ alkoxyalkyl group, a C₁₋₃₀alkoxycarbonylalkyl group, a C₁₋₃₀ alkylcarbonylalkyl group, a C₁₋₃₀cycloalkylcarbonylalkyl group, a C₁₋₃₀ cyanoalkyl group, a C₁₋₃₀dialkylaminocarbonylalkyl group, a C₁₋₃₀ dialkylaminoalkyl group, aC₁₋₃₀ dialkylaminosulfonylalkyl group, a C₁₋₃₀ azidoalkyl group, abenzyl group, a phenyl group, a nitro group, a cyano group, an azidegroup, an amino group, a C₁₋₃₀ monoalkylamino group, a C₁₋₃₀dialkylamino group, a benzylamino group, an C₁₋₃₀ alkylcarbonylaminogroup which may be substituted by a halogen atom, a benzoylamino group,a C₁₋₃₀ alkoxycarbonylamino group, a phenoxycarbonylamino group, a C₁₋₃₀alkylsulfonylamino group wherein the amino group may be substituted by aC₁₋₃₀ alkyl group, a phenylsulfonylamino group wherein the amino groupmay be substituted by an C₁₋₃₀ alkyl group, a C₁₋₃₀ alkylideneaminogroup, a benzylideneamino group, a tetrazolyl group which may besubstituted with methyl, a group of the formula --COR⁴,wherein R⁴ is ahydrogen atom, a hydroxyl group, a C₁₋₃₀ alkyl group, a C₁₋₃₀ cycloalkylgroup, a C₁₋₃₀ haloalkyl group, a C₂₋₂₀ alkenyl group, a C₂₋₂₀ alkynylgroup, a benzyl group, a phenyl group, a C₁₋₃₀ alkoxy group, a C₁₋₃₀haloalkoxy group, an C₁₋₃₀ alkoxyalkoxy group, a C₂₋₂₀ alkenyloxy group,a C₁₋₃₀ haloalkenyloxy group, a C₂₋₂₀ alkynyloxy group, a benzyloxygroup or a phenoxy group, a group of the formula --C(O)NR⁵ R⁶,wherein R⁵and R⁶ are, independently, a hydrogen atom, an C₁₋₃₀ alkyl group, aC₂₋₂₀ alkenyl group, a C₂₋₂₀ alkynyl group, a benzyl group, a phenylgroup or a C₁₋₃₀ alkoxy group, and a group of the formula --SR⁷,whereinR⁷ is a hydrogen atom, a C₁₋₃₀ alkyl group or a halo(C₁₋₃₀)alkyl group,a group of the formula --SO₂ NR⁵ R⁶,wherein R⁵ and R⁶ have the samemeanings as defined above, a group of the formula --S(O)^(n) R⁸,whereinn represents an integer of 1 or 2, and R⁸ represents a C₁₋₃₀ alkylgroup, a C₂₋₂₀ alkenyl group or a halo(C₁₋₃₀)alkyl group, a group of theformula --OR⁹,wherein R⁹ is a hydrogen atom, a C₁₋₃₀ alkyl group, a C₃cycloalkyl(C₁₋₃₀)alkyl group, a C₁₋₃₀ alkenyl group, a C₁₋₃₀ alkynylgroup, a benzyl group, wherein said benzyl group may be substituted by ahalogen atom, a C₁₋₃₀ alkyl group or a C₁₋₃₀ alkoxy group and, ahalo(C₁₋₃₀)alkyl group, a halo(C₁₋₃₀) alkenyl group, a phenyl groupsaidphenyl group may be substituted by a halogen atom, a C₁₋₃₀ alkyl groupor a C₁₋₃₀ alkoxy group, a C₁₋₃₀ alkoxyalkyl group, a C₁₋₃₀alkoxyalkoxyalkyl group, a C₁₋₃₀ haloalkoxyalkyl group, a C₁₋₃₀benzyloxyalkyl group, a C₁₋₃₀ phenoxyalkyl group, a C₁₋₃₀ alkylthioalkylgroup, a C₁₋₃₀ dialkylaminoalkyl group, an C₁₋₃₀ azidoalkyl group, aC₁₋₃₀ alkylcarbonyl group, a C₁₋₃₀ haloalkylcarbonyl group, a benzoylgroup, a C₁₋₃₀ dialkylaminocarbonyl group, a cyanoalkyl group, a C₁₋₃₀alkylideneamino group, a C₁₋₃₀ dialkylideneamino group, abenzylideneamino group or a C₁₋₃₀ alkoxycarbonylalkyl group,or theformula --C(═NOR¹⁰)R¹¹, wherein R¹⁰ represents a hydrogen atom, a C₁₋₃₀alkyl group, a C₂₋₂₀ alkenyl group, a C₂₋₂₀ alkynyl group, a benzylgroup, a C₁₋₃₀ haloalkyl group or a phenyl C₁₋₃₀ group, and R¹¹represents a hydrogen atom, a alkyl group, a benzyl group, a C₁₋₃₀haloalkyl group or a phenyl group, R² and R³ may together be --O--C₂ H₄--O--, --S--C₂ H₄ --S-- or --O--CH₂ --O--; A and B are, independently,C₁₋₃₀ alkyl group, a C₁₋₃₀ haloalkyl group, a C₁₋₃₀ alkoxy group, aC₁₋₃₀ monoalkylamino group, a C₁₋₃₀ dialkylamino group, a halogen atomor a C₁₋₃₀ haloalkoxy group, Z is a methine group; X is an oxygen atomor a sulfur atom; and Y is a hydrogen atom, a C₁₋₃₀ alkyl group or aC₁₋₃₀ alkoxyalkyl group.
 2. An indazolesulfonylurea derivative of theformula: ##STR80## wherein R¹ is a hydrogen atom, a C₁₋₃₀ alkyl group ora C₂₋₂₀ alkenyl group;R² and R³ are, independently, a hydrogen atom, ahalogen atom, a C₁₋₃₀ alkyl group, a C₁₋₃₀ alkoxy group, a C₁₋₃₀haloalkoxy group, a C₁₋₃₀ alkylthio group, a C₁₋₃₀ alkylsulfinyl group,a C₁₋₃₀ alkylsulfonyl group, a C₁₋₃₀ alkoxycarbonyl group, a C₁₋₃₀dialkylaminocarbonyl group, a nitro group or a cyano group; A and B are,independently, a C₁₋₃₀ alkyl group, a C₁₋₃₀ alkoxy group or a halogen;and Z is a methine group.
 3. An indazolesulfonylurea derivative of theformula: ##STR81## wherein R¹ is a hydrogen atom, a C₁₋₃₀ alkyl group ora phenyl group;R² and R³ are, independently, a hydrogen atom, a halogenatom, a C₁₋₃₀ alkyl group, a hydroxyl group, a C₁₋₃₀ alkoxy group, aC₁₋₃₀ haloalkenyloxy group, an C₁₋₃₀ alkoxycarbonylalkoxy group, a C₁₋₃₀cycloalkylalkoxy group, a C₁₋₃₀ dialkylaminoalkoxy group, a C₁₋₃₀alkoxyalkoxy group, a C₁₋₃₀ haloalkoxy group, a C₂₋₂₀ alkynyloxy group,a C₁₋₃₀ alkenyloxy group, a C₁₋₃₀ alkylthio group, a C₁₋₃₀ alkylsulfonylgroup, a C₁₋₃₀ alkoxycarbonyl group, a C₁₋₃₀ dialkylaminocarbonyl group,a nitro group, a cyano group, a C₁₋₃₀ monoalkylamino group, a C₁₋₃₀dialkylamino group or a benzylamino group; A and B are, independently, aC₁₋₃₀ alkyl group, a C₁₋₃₀ alkoxy group or a halogen atom; and Z is amethine group.
 4. A herbicidal composition comprising anindazolesulfonylurea as defined in claim 1 and an inert carrier.